List of Publications

2026

370 Development of a random background to understand ligand optimization. Xinyu Xu, Olivier Mailhot, Galen J. Correy, Xi-Ping Huang, Joao M. Braz, Da Shi, Karthik Srinivasan, Kara Zielinski, Yuliia Holota, Yuliia Kuziv, Christos Iliopoulos-Tsoutsouvas, Nathan D. Levinzon, Yagmur U. Doruk, Moira M. Rachman, Morgan E. Diolaiti, Maisie G. V. Stevens, Fangyu Liu, Katie L. Holland, Harald Hübner, Jing Wang, Yujin Wu, Alan Ashworth, Alexandros Makriyannis, Yuqi Zhang, Yurii S. Moroz, Peter Gmeiner, Robert Abel, Aashish Manglik, Allan I. Basbaum, Bryan L. Roth, James S. Fraser, Brian Shoichet. Nature 2026, accepted. doj>10.1038/s41586-026-11013-5

369 Development of covalent agonists for the muscarinic acetylcholine receptor. Katrin Eitel, Philipp Risel, Jonas Kaindl, Jürgen Einsiedel, Harald Hübner, Peter Gmeiner. Bioorg. Med. Chem. 2026, 143, 118783. doj>10.1016/j.bmc.2026.118783.

368 Development of pH-Sensitive β-Adrenergic Receptor Antagonists. Tobias Braun, Theresa Pröll, Nils Weißing, Harald Hübner, Peter Gmeiner. ACS Pharmacol. Transl. Sci 2026. doi>10.1021/acsptsci.6c00296.

367  Docking of virtual libraries identifies small-molecule agonists of neurotensin receptors with analgesic activity.Nicolas Panel, Duy Duc Vo, Harald Hübner, Mattia Delugi, Szymon Pach, Félix Bélair, Dorothée Weikert, Christoph Klenk, Mark Hilge, Niharika Shiva, Isabelle Brochu, Jean-Michel Longpré, Frida Bällgren, Aljona Saleh, Huabin Hu, Jon Kapla, Stefanie Kampen, Israel Cabeza de Vaca, Jan Kihlberg, Nina Wettschureck, Philippe Sarret, Andreas Plückthun, Peter Gmeiner, Jens Carlsson. Nat. Commun. 2026, 17, 6970. doi>10.1038/s41467-026-74990-1.

366  Neurotensin receptor 2 agonism attenuates adverse cardiac remodeling in preclinical models. Niharika Shiva, Haruya Kawase, Jürgen Einsiedel, Jeonghyeon Kwon, Shamit Kumar, Jingchen Shao, Zhaoyu Du, Natalia Kubin, Miho Shimari, Stefan Günther, Tiangang Li, Pieterjan Dierickx, Samuel Sossalla, Stefan Offermanns, Peter Gmeiner, Nina Wettschureck. Sci Transl. Med. 2026, 18, eaea9877. [doi>10.1126/scitranslmed.aea9877] .

365  A Selectfluor-based Polonovski Rearrangement Leading to Novel Entities for Synthetic and Medicinal Applications. Jakob Kuhn, Susanne Gradl, Vanessa Osterloh, Peter Gmeiner, Harald Hübner, Markus R. Heinrich. Chem. Eur. J. 2026, e71318.[doi>/10.1002/chem.71318] 

364 Large Library Docking for Polypharmacology. Yujin Wu, Seth Vigneron, Joao Braz, Karthik Srinivasan, Elissa A. Fink, Xi-Ping Huang, Xinyu Xu, Harald Huebner, Joseph Y. Kim, Jing Wang, Tara Pfeiffer, Kensuke Sakamoto, Dmytro S. Radchenko, Ramona M. Rodriguiz, Yurii S. Moroz, John J. Irwin, Peter Gmeiner, Christian Billesboelle, Bryan L. Roth, Allan I. Basbaum, Aashish Manglik, William C. Wetsel, Brian K. Shoichet. J. Med. Chem. 2026, 69, 6210-6229. [doi>10.1021/acs.jmedchem.5c03810] 

363 The Role of Intrinsically Disordered Domains in Regulation G Protein-Coupled Receptor Signaling. Jun Xu, Ruoyi Qiu, Alexander M. Carces, Harald Huebner, Xinyu Xu, Chengyu Hao, Dorothee Weikert, Peter Gmeiner, Michael T. Lerch, Brian K. Kobilka. J. Am. Chem. Soc. 2026, 148, 1, 1430-1443. [doi>10.1021/jacs.5c17796]

2025

362 SAG1.3-derived Frizzled-targeting small molecule compounds. Lukas Graetz, Ainoleena Turku, Pawel Kozielewicz, Carl-Fredrik Bowin, Magdalena M., Scharf, Jan H. Voss, Julia Kinsolving, Rawan Shekhani, Nuria Oliva-Vilarnau, Tobias, Koolmeister, Marlies Koerber, Volker M. Lauschke, Stefan Loeber, Peter Gmeiner, Gunnar Schulte. J. Biol. Chem. 301, 2025,110751. [doi>10.1016/j.jbc.2025.110751 

361 Invention of 1-acyl-3-aminoindazoles for treating cystic fibrosis. Brian Shoichet, Peter Gmeiner, Jue Chen. WO2024178219 A1 (2024). 

360 Mechanism and function of GPR3 regulated by a negative allosteric modulator. Geng Chen, Jana Blahova, Nico Staffen, Harald Huebner, Nadja Nunhoefer, Chen Qiu, Peter Gmeiner, Dorothee Weikert, Yang Du, Jun Xu. Nat. Commun. 2025, 16, 7988. 297, 117964. [doi>10.1038/s41467-025-63422-1]

359 A Warm Welcome to MedChem: The Frontiers in Medicinal Chemistry 2025. Matthias Schiedel, Marta Pinto, Andrea Unzue Lopez, Philipp Barbie, Felix Pape, Anika Tarasewicz, Gerhard Hessler, Peter Gmeiner, Christina Lamers, Matthias Gehringer. ChemMedChem. 2025, 000, e2500609. [doi>10.1002/cmdc.202500609] 

358 Hunting for lubeluzole analogues as antimyotonic agents with reduced cardiac liability. Maria Maddalena Cavalluzzi, Roberta Gualdani, Alessandro Farinato, Concetta Altamura, Sabata Pierno, Natalie Paola Rotondo, Francesco Terlizzi, Laura Beatrice Mattioli, Maria Grazia Perrone, Maria Cristina Lomuscio, Giuseppe Felice Mangiatordi, Nicola Antonio Colabufo, Antonio Carrieri, Roberta Budriesi, Peter Gmeiner, Harald Huebner, Jean-Francois Desaphy, Giovanni Lentini. Eur. J. Med. Chem, 2025, 297,117964. [doi>10.1016/j.ejmech.2025.117964] 

357 Discovery of a functionally selective serotonin receptor (5-HT_1AR) agonist for the treatment of pain. Annika Ullrich, Johannes Schneider, Joao M. Braz, Eduard Neu, Nico Staffen, Markus Stanek, Jana Blahova, Tamsanqa Hove, Tamara Albert, Stefan Loeber, Karnika Bhardwaj, Sian Rodriguez-Rosado, Elissa Fink, Tim Rasmussen, Harald Huebner, Asuka Inoue, Brian K. Shoichet, Allan I. Basbaum, Bettina Boettcher, Dorothee Weikert, Peter Gmeiner. Sci. Adv. 11, 2025, 25 eadv9267. [doi>10.1126/sciadv.adv9267] 

356 Towards „unmakable“ psychedelics: SAR exploration of psilocin analogs obtained by a HATU-mediated amide coupling strategy. Judith Stirn, Raphael Berger, Harald Huebner, Peter Gmeiner, Christian D. Klein. EJMCR, 2025, 15, 100278. [doi>10.1016/j.ejmcr.2025.100278] 

355 ^99mTc-Labeled Diarylpyrazoles for Single-Emission Computer Tomography Imaging of Neurotensin Receptor-Positive Tumors: A Comparative Preclinical Study. Roman Potemkin, Simone Maschauer, Harald Huebner, Torsten Kuwert, Tobias Baeuerle, Peter Gmeiner, Olaf Prante. Pharmaceutics, 2025. 17, 6, 700. [doi>10.3390/pharmaceutics17060700] 

354 Neurotensin (8-13) analogs targeting NTS1 and NTS2 receptors: A comparative in vitro and molecular modeling study. Kiril Kirilov, Maria Ponticelli, Toni Kuehl, Harald Huebner, Maya G. Georgieva, Matthias Vogel, Aneliya A. Balacheva, Bodo Haas, Tamara I. Pajpanova, Maima Matin, Luigi Milella, Peter Gmeiner, Diana Imhof, Nikolay T. Tzvetkov. Curr. Res. Biotechnol. 2025, 9, 110298. [doi>10.1016/j.crbiot.2025.100290] 

353 Identification of an a-factor-like pheromone secreted by the heterothallic ascomycete Aspergillus fumigatus. Sven Krappmann, Elisabeth Gabl, Tobias Pazen, Anna Heizmann, Stefanie Poeggeler, Thomas Krueger, Olaf Kniemeyer, Juergen Einsiedel, Peter Gmeiner, Yidong Yu, Paul S. Dyer, Scott E. Baker, Minou Nowrousian. Curr. Biol. 2025, 35,10,2414-2423.e5. In Press. [doi>10.1016/j.cub.2025.03.080] 

352 Synthesis and Characterization of Photoswitchable Covalent Ligands for the beta2-Adrenoceptor. Ulrike Wirth, Eduard Neu, Davide Provasi, Steffen Feustel, Maximilian F. Schmidt, Harald Huebner, Dorothee Weikert, Marta Filizola, Burkhard Koenig, Peter Gmeiner. Angew. Chem. Int. Ed. 2025,Ed. 64,e2024240038. [doi>10.1002/anie.202424038] 

351 Acid sphingomyelinase activity suggests a new antipsychotic pharmaco-treatment strategy for schizophrenia. Daria Chestnykh, Christiane Muehle, Fabian Schumacher, Liubov S. Kalinichenko, Stefan Loeber, Peter Gmeiner, Christian Alzheimer, Stephan von Hoersten, Burkhard Kleuser, Steffen Uebe, Arif B. Ekici, Erich Gulbins, Johannes Kornhuber, Hee Kyung Jin, Jae-sung Bae, Anbarasu Lourdusamy & Christian P. Mueller. Mol Psychiatry 2025, 30, 2891-2906. [doi>10.1038/s41380-025-02893-6] 

350 Structure and dynamics determine G protein coupling specificity at a class A GPCR. Marina Casiraghi, Haoqing Wang, Patrick C. Brennan, Chris Habrian, Harald Huebner, Maximilian F. Schmidt, Luis Maul, Biswaranjan Pani, Sherif M. F. M. Bahriz, Bing Xu, Nico Staffen, Tufa E. Assafa, Bohan Chen, Elizabeth White, Roger K. Sunahara, Asuka Inoue, Yang K. Xiang, Robert J. Lefkowitz, Ehud Y. Isacoff, Nathaniel Nucci, Peter Gmeiner, Michael T. Lerch, and Brian K. Kobilka. Sci. Adv. 11, 2025, eadq3971. [doi>10.1126/sciadv.adq3971.] 

2024

349 A Putative Frizzled 7 Targeting Compound Acts as a Firefly Luciferase Inhibitor. Julia Kinsolving, Lukas Graetz, Jan Hendrik Voss, Bente Loew, Emily Shorter, Baptiste Jude, Johanna T. Lanner, Stefan Loeber, Peter Gmeiner, Gunnar Schulte. J. Med. Chem. 2024, 67, 22332-22341. [doi>10.1021/acs.jmedchem.4c02766] 

348 A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR. Lior Peri, Donna Maatzov, Dominic R. Huxley, Alon Rainish, Fabrizio Fierro, Liel Sapir, Tara Pfeiffer, Lukas Waterloo, Harald Huebner, Yoav Peleg, Peter Gmeiner, Peter J. McCormick, Dorothee Weikert, Masha Y. Niv, Moran Shalev-Benami. Nat. Commun. 2024, 15, 9991. [doi>10.1038/s41467-024-54157-6] 

347 Heteroaryl derivatives of suvorexant as OX1R selective PET ligand candidates: Cu-mediated ¹⁸F-fuorination of boroxines, in vitro and initial in vivo evaluation. Kim-Viktoria Bolik, Jan Hellmann, Simone Maschauer, Eduard Neu, Juergen Einsiedel, Patrick Riss, Nora Vogg, Joerg Koenig, Martin F. Fromm, Harald Huebner, Peter Gmeiner, Olaf Prante. EJNMMI Res. 2024, 14, 80. [doi>10.1186/s13550-024-01141-2] 

346 Structure-guided discovery of orexin receptor-binding PET ligands. Katharina Distler, Simone Maschauer, Euard Neu, Harald Huebner, Juergen Einsiedel, Olaf Prante, Peter Gmeiner. Bioorg. Med. Chem. 2024, 110, 117823. [doi>10.1016/j.bmc.2024.117823] 

345 Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays. Fabian J. Ertl, Sergei Kopanchuk, Nicola C. Dijon, Santa Veiksina, Maris-Johanna Tahk, Tonis Laasfeld, Franziska Schettler, Albert O. Gattor, Harald Huebner, Nataliya Archipowa, Johannes Koeckenberger, Markus R. Heinrich, Peter Gmeiner, Roger J. Kutta, Nicholas D. Holliday, Ago Rinken, Max Keller. J. Med. Chem. 2024, 67,16664-16691. [doi>10.1021/acs.jmedchem.4c01470] 

344 Design, Synthesis, and Characterization of New Delta Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors. Antonios Drakopoulos, Zsombor Koszegi, Kerstin Seier, Harald Huebner, Damien Maurel, Remy Sounier, Sebastien Granier, Peter Gmeiner, Davide Calebiro, Michael Decker. J. Med. Chem. 2024, 67, 12618-12631. [doi>10.1021/acs.jmedchem.4c00627] 

343 Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. Hannah Vogt, Patrick Shinkwin, Max E. Huber, Nico Staffen, Harald Huebner, Peter Gmeiner, Matthias Schiedel, Dorothee Weikert. ACS Pharmacol. Transl. Sci. 2024, 7, 1533-1545. [doi>10.1021/acsptsci.4c00086] 

342 Structure-based discovery of CFTR potentiators and inhibitors. Fangyu Liu, Anat Levit Kaplan, Jesper Levring, Juergen Einsiedel, Stephanie Tiedt, Katharina Distler, Natalie S. Omattage, Ivan S. Kondratov, Yurii S. Moroz, Harlan L. Pietz, John J. Irwin, Peter Gmeiner, Brian K. Shoichet, Jue Chen. Cell 2024, 187. [doi>10.1016/j.cell.2024.04.046] 

341 Covalent and Visible-Light Photoswitchable Derivatives of the Potent Synthetic Opioid Isotonitazene and Other Nitazenes. Ranit Lahmy, Harald Huebner, Peter Gmeiner, Burkhard Koenig. ChemPhotoChem 2024, e202400022. [doi>10.1002/cptc.202400022] 

340 Time-resolved cryo-EM of G-protein activation by a GPCR. Makaia M. Papasergi-Scott, Guillermo Perez-Hernandez, Hossein Batebi, Yang Gao, Goezde Eskici, Alpay B. Seven, Ouliana Panova, Daniel Hilger, Marina Casiraghi, Feng He, Luis Maul, Peter Gmeiner, Brian K. Kobilka, Peter W. Hildebrand, Georgios Skiniotis. Nature 2024, 629, 1182-1191. [doi>10.1038/s41586-024-07153-1] 

339 The small molecule activator S3969 stimulates the epithelial sodium channel (ENaC) by interacting with a specific binding pocket in the channel’s beta-subunit. Florian Sure, Juergen Einsiedel, Peter Gmeiner, Patrick Duchstein, Dirk Zahn, Christoph Korbmacher, Alexandr V. Ilyaskin. J Biol Chem 2024, 300, 4, 105785. [doi>10.1016/j.jbc.2024.105785] 

338 Structural and functional characterization of the endogenous agonist for orphan receptor GPR3. Geng Chen, Nico Staffen, Zhangsong Wu, Xinyu Xu, Jinheng Pan, Asuka Inoue, Tingyi Shi, Peter Gmeiner, Yang Du, Jun Xu. Cell Res. 2024, 34, 262-265. [doi>10.1038/S41422-023-00919-8] 

337 Photo-Adrenalines: Photoswitchable beta2-Adrenergic Receptor Agonists as Molecular Probes for the Study of Spatiotemporal Adrenergic Signaling. Alexandra Sink, Hubert Gerwe, Harald Huebner, Valerie Boivin-Jahns, Julia Fender, Kristina Lorenz, Peter Gmeiner, Michael Decker. Chem. EUR. J. 2024, 30, 11, e202303506. [doi>10.1002/chem.202303506] 

2023

336 Development of Photoswitchable Tethered Ligands that Target the mu-Opioid Receptor. Ranit Lahmy, Harald Huebner, Daniel Lachmann, Peter Gmeiner, Burkhard Koenig. ChemMedChem 2023, 18,  23, e202300228. [doi>10.1002/cmdc.202300228] 

335 Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists. Fabian Grassl, Leonard Bock, Alvaro Huete-Huerta Gonzalez, Martin Schiller, Peter Gmeiner, Joerg Koenig, Martin F. Fromm, Harald Huebner, Markus Heinrich. J. Med. Chem. 2023, 66, 14, 9710-9730 . [doi>110.1021/acs.jmedchem.3c00537] 

334 Identification and quantification of kukoamine A and kukoamine B as novel mu-opioid receptor agonists in potato and other solanaceous plants. Julia Saller, Carina List, Harald Huebner, Peter Gmeiner, Timothy Clark, Monika Pischetsrieder. Food. Chem. 2023, 427, 136637. [doi>10.1016/j.foodchem.2023.136637]

333 The beer component hordenine inhibits alcohol addiction-associated behaviours in mice. Yan Li, Christina Vogel, Liubov S. Kalinichenko, Harald Huebner, Dorothee Weikert, Natascha Schaefer, Peter Gmeiner, Carmen Villmann, Monika Pischetsrieder, Christian P. Mueller. Addict. Biol. 2023, 28, 8, e13305.[doi>10.1111/adb.13305] 

332 Alpha-2a adrenergic receptor modulators and uses thereof. Peter Gmeiner, Harald Huebner, Philipp Seemann, Tara Pfeiffer, Yang Du, Jun Xu, Brian K. Shoichet, Elissa A. Fink, Allan J. Basbaum, Joao M. Braz WO 2023081800 A1, PCT Int. Appl. (2023). 

331 Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief. Alan Hegron, Chloe J. Peach, Raquel Tonello, Philipp Seemann, Shavonne Teng, Rocco Latorre, Harald Huebner, Dorothee Weikert, Jeanette Rientjes, Nicholas A. Veldhuis, Daniel P. Poole, Dane D. Jensen, Alex R. B. Thomsen, Brian L. Schmidt, Wendy L. Imlach, Peter Gmeiner, Nigel W. Bunnett. PNAS 2023, 120, 22, e2220979120. [doi>10.1073/pnas.2220979120] 

330 Selectfluor-Mediated Chlorination and Fluorination of Arenes: Late-Stage Functionalization of APIs and Its Biological Effects. Susanne Gradl, Viviane Zantop, Peter Gmeiner, Harald Huebner, Markus R. Heinrich. ChemMedChem 2023, 18,15, e20230144. [doi>10.1002/cmdc.202300144]

329 Constrained catecholamines gain beta2AR selectivity through allosteric effects on pocket dynamics. Xinyu Xu, Jeremy Shonberg, Jonas Kaindl, Mary Clark, Anne Stoessel, Luis Maul, Daniel Mayer, Harald Huebner, Kunio Hirata, AJ Venkatakrishnan, Ron Dror, Brian Kobilka, Roger Sunahara, Xiangyu Liu, and Peter Gmeiner. Nat. Commun. 2023, 14, 2138. [doi>10.1038/s41467-023-37808-y]

328 Neurotensin 8-13 analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinsons disease. Toni Kuehl, Maya G. Georgieva, Harald Huebner, Maria Lazarova, Matthias Vogel, Bodo Haas, Martina I. Peeva, Aneliya A. Balacheva, Ivan P. Bogdanov, Luigi Milella, Maria Ponticelli, Tsvetomir Garev, Immacolata Faraone, Roumyana Detcheva, Borislav Minchev, Polina Pekkova-Kirova, Lyubka Tancheva, Reni Kalfin, Atanas G. Atanasov, Liudmil Antonov, Tamara I. Pajpanova, Kiril Kirilov, Marcus Gastreich, Peter Gmeiner, Diana Imhof, Nikolay T. Tzvetkov. Eur. J. Med. Chem. 2023, 254, 115386. [doi>10.1016/j.ejmech.2023.115386 

327 Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands. Fabrizio Fierro, Lior Peri, Harald Huebner, Alina Tabor-Schkade, Lukas Waterloo, Stefan Loeber, Tara Pfeiffer, Dorothee Weikert, Tamir Dingjan, Eitan Margulis, Peter Gmeiner, Masha Y Niv. Cell. Mol. Life Sci. 2023, 80, 114. [doi>10.1007/s00018-023-04765-] 

326 Design of Drug Efficacy Guided by Free Energy Simulations of the beta2-Adrenoceptor. Nicolas Panel, Duc Duy Vo, Nour Aldin Kahlous, Harald Huebner, Stephanie Tiedt, Pierre Matricon, Jody Pacalon, Oliver Fleetwood, Stefanie Kampen, Andreas Luttens, Lucie Delemotte, Jan Kihlberg, Peter Gmeiner, Jens Carlsson. Angew. Chem. Int. Ed. 2023, e202218959. [doi>10.1002/anie.202218959]

325 Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14. Lukas Waterloo, Harald Huebner, Fabrizio Fierro, Tara Pfeiffer, Regine Brox, Stefan Loeber, Dorothee Weikert, Masha Y. Niv, Peter Gmeiner. J. Med. Chem. 2023, 66, 5, 3499-3521. [doi>10.1021/acs.jmedchem.2c01997]

324 Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor. Jun Xu, Qinggong Wang, Harald Huebner, Yunfei Hu, Xiaogang Niu, Haoqing Wang, Shoji Maeda, Asuka Inoue, Yuyong Tao, Peter Gmeiner, Yang Du, Changwen Jin, Brian K. Kobilka. Nat. Commun. 2023, 14, 376. [doi>10.1038/s41467-022-35726-z] 

323 Phosphoproteomic Analysis of Dopamine D2 Receptor Signaling Reveals Interplay of G Protein- and beta-Arrestin-Mediated Effects. Deborah Wenk, Shahbaz Khan, Vladimir Ignatchenko, Harald Huebner, Peter Gmeiner, Dorothee Weikert, Monika Pischetsrieder, Thomas Kislinger. J. Proteome Res. 2023, 22, 1, 259-271. [doi>10.1021/acs.jproteome.2c00707]

2022

322 Synthesis, Characterization, and Application of Muscarinergic M3 Receptor Ligands Linked to Fluorescent Dyes. Johannes Koeckenberger, Oliver Fischer, Andreas Konopa, Sebastian Bergwinkl, Susanne Muehlich, Peter Gmeiner, Roger Jan Kutta, Harald Huebner, Max Keller, Markus R. Heinrich. J. Med. Chem. 2022, 65, 16494-16509. [doi>10.1021/acs.jmedchem.2c01376]

321 Structure-based discovery of nonopioid analgesics acting through the alpha2A-adrenergic receptor. Elissa A. Fink, Jun Xu, Harald Huebner, Joao M. Braz, Philipp Seemann, Charlotte Avet, Veronica Craik, Dorothee Weikert, Maximilian F. Schmidt, Chase M. Webb, Nataliya A. Tolmachova, Yurii S. Moroz, Xi-Ping Huang, Chakrapani Kalyanaraman, Stefan Gahbauer, Geng Chen, Zheng Liu, Matthew P. Jacobson, John J. Irwin, Michel Bouvier, Yang Du, Brian K. Shoichet, Allan I. Basbaum, Peter Gmeiner. Science 2022, 377, eabn7065. [doi>10.1126/science.abn7065] 

320 Photochromic Fentanyl Derivatives for Controlled mu-opioid Receptor Activation. Ranit Lahmy, Harald Huebner, Maximilian F. Schmidt, Daniel Lachmann, Peter Gmeiner, Burkhard Koenig. Chem. Eur. J. 2022, e202201515. [doi>10.1002/chem.202201515] 

319 The Bitter Taste Receptor TAS2R14 as a Drug Target. Lukas A. W. Waterloo, Stefan Loeber, Peter Gmeiner. Chimia 2022, 76, 418-424. [doi>10.2533/chimia.2022.418] 

318 Activation and allosteric regulation of the orphan GPR88-Gi1 signaling complex. Geng Chen, Jun Xu, Asuka Inoue, Maximilian Schmidt, Chen Bai, Qiuyuan Lu, Peter Gmeiner, Zheng Liu, Yang Du. Nat. Commun. 2022, 13:2375. [doi>10.1038/s41467-022-30081-5] 

317 Structure-Based Evolution of G Protein-Biased mu-Opioid Receptor Agonists. Haoqing Wang, Florian Hetzer, Weijiao Huang, Qianhui Qu, Justin Meyerowitz, Jonas Kaindl, Harald Huebner, Georgios Skiniotis, Brian K. Kobilka, Peter Gmeiner. Angew. Chem. 2022, e202200269. [doi>10.1002/ange.202200269] Angew. Chem. Int. Ed. 2022, e202200269. [doi>10.1002/anie.202200269] 

316 Substituted vicinal diamine compounds and their use in the treatment, amelioration or prevention of pain. Peter Gmeiner, Harald Huebner, Florian Hetzer. WO 2022048922 A1, PCT Int. Appl. (2022). 

315 Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors. Juergen Einsiedel, Maximilian F. Schmidt, Harald Huebner, Peter Gmeiner. Bioorg. Med. Chem. 2022, 61, 116720. [doi>10.1016/j.bmc.2022.116720] 

314 Structural insights into ligand recognition, activation, and signaling of the alpha2A adrenergic receptor. Jun Xu, Sheng Cao, Harald Huebner, Dorothee Weikert, Geng Chen, Qiuyuan Lu, Daopeng Yuan, Peter Gmeiner, Zheng Liu, Yang Du. Sci. Adv. 2022, 8, eabj5347. [doi>10.1126/sciadv.abj5347] 

2021

313 N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y4 Receptor Ligands Results in Picomolar Binding Constants. Adam Konieczny, Marcus Conrad, Fabian J. Ertl, Jakob Gleixner, Albert O. Gattor, Lukas Graetz, Maximilian F. Schmidt, Eduard Neu, Anselm H. C. Horn, David Wifling, Peter Gmeiner, Timothy Clark, Heinrich Sticht, and Max Keller. J. Med. Chem. 2021, 64, 16746-16769. [doi>10.1021/acs.jmedchem.1c01574] 

312 Functional Reconstitution of Dopamine D2 Receptor into a Supported Model Membrane in a Nanometric Confinement. Rurika Nagai, Ayane Sugimachi, Yasushi Tanimoto, Kenichi G. N. Suzuki, Fumio Hayashi, Dorothee Weikert, Peter Gmeiner, Rinshi S. Kasai, Kenichi Morigaki. Advanced Biology 2021, 2100636. [doi>10.1002/adbi.202100636] 

311 Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer. Julian Budzinski, Simone Maschauer, Hiroyuki Kobayashi, Pierre Couvineau, Hannah Vogt, Peter Gmeiner, Anna Roggenhofer, Olaf Prante, Michel Bouvier, Dorothee Weikert. Commun. Biol. 2021, 4, 1062. [doi>10.1038/s42003-021-02574-4] 

310 Optimizing the Expression of Human Dopamine Receptors in Escherichia coli. Vanessa Boritzki, Harald Huebner, Anni Allikalt, Peter Gmeiner, Birgitta M. Woehrl. Int. J. Mol. Sci. 2021, 22, 8647-8661. [doi>10.3390/ijms22168647]

309 Abolishing Dopamine D2long/D3 Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H2 Receptor Agonists. Katharina Tropmann, Merlin Bresinsky, Lisa Forster, Denise Moennich, Armin Buschauer, Hans-Joachim Wittmann, Harald Huebner, Peter Gmeiner, Steffen Pockes, Andrea Strasser. J. Med. Chem. 2021, 64, 8684-8709. [doi>10.1021/acs.jmedchem.1c00692] 

308 Visualization of beta-adrenergic receptor dynamics and differential localization in cardiomyocytes. Marc Bathe-Peters, Philipp Gmach, Horst-Holger Boltz, Juergen Einsiedel, Michael Gotthardt, Harald Huebner, Peter Gmeiner, Martin J. Lohse, Paolo Annibale. PNAS 2021, 118, e2101119118. [doi>10.1073/pnas.2101119118]

307 Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M2R selectivity. Corinna. G. Weinhart, David Wifling, Maximilian F. Schmidt, Eduard Neu, Carina Hoering, Timothy Clark, Peter Gmeiner, Max Keller. Eur. J. Med. Chem. 2021, 213, 113159. [doi>10.1016/j.ejmech.2021.113159] 

306 Functionally selective activation of the dopamine receptor D2 is mirrored by the protein expression profiles. Deborah Wenk, Vladimir Ignatchenko, Andrew Macklin, Harald Huebner, Peter Gmeiner, Dorothee Weikert, Monika Pischetsrieder, Thomas Kislinger. Sci. Rep. 2021, 11, 3501. [doi>10.1038/s41598-021-83038-x] 

305 Sensitization to amphetamine psychostimulant effect: A key role for ventral tegmental area neurotensin type 2 receptors and MAP kinase pathway. David Voyer, Juergen Einsiedel, Peter Gmeiner, Daniel Levesque, Pierre-Paul Rompre. Addict. Biol. 2021, e13008. [doi>10.1111/adb.13008] 

304 Homobivalent Dopamine D2 Receptor Ligands Modulate the Dynamic Equilibrium of D2 Monomers and Homo- and Heterodimers. Tamara Ullmann, Marie Gienger, Julian Budzinski, Jan Hellmann, Harald Huebner, Peter Gmeiner, Dorothee Weikert. ACS Chem. Biol. 2021, 16, 371-379. [doi>10.1021/acschembio.0c00895] 

303 Presynaptic vesicular accumulation is required for antipsychotic efficacy in psychotic-like rats. Taygun Uzuneser, Eva-Maria Weiss, Jana Dahlmanns, Liubov Kalinichenko, Davide Amato, Johannes Kornhuber, Christian Alzheimer, Jan Hellmann, Jonas Kaindl, Harald Huebner, Stefan Loeber, Peter Gmeiner, Teja Groemer, Christian Mueller. J. Psychopharmacol. 2021, 35, 65-77. [doi>10.1177/0269881120965908] 

302 Binding pathway determines norepinephrine selectivity for the human Beta1AR over Beta2AR. Xinyu Xu, Jonas Kaindl, Mary J. Clark, Harald Huebner, Kunio Hirata, Roger K. Sunahara, Peter Gmeiner, Brian K. Kobilka, Xiangyu Liu. Cell Res. 2021, 31, 569-579. [doi>10.1038/s41422-020-00424-2] Supp. Info

301 Radiosynthesis and evaluation of ¹⁸F-labeled dopamine D4-receptor ligands. Michael Willmann, Johannes Ermert, Olaf Prante, Harald Huebner, Peter Gmeiner, Bernd Neumaier. Nucl. Med. Biol. 2021, 92, 43-52. [doi>10.1016/j.nucmedbio.2020.07.004] 

2020

300 Fluorescent ligands for dopamine D2/D3 receptors. Anni Allikalt, Nirupam Purkayastha, Khajidmaa Flad, Maximilian F. Schmidt, Alina Tabor, Peter Gmeiner, Harald Huebner, Dorothee Weikert. Sci. Rep. 2020, 10, 21842. [doi>10.1038/s41598-020-78827-9] 

299 Pharmacological characterization of low-to-moderate affinity opioid receptor agonists and brain imaging with 18F-labeled derivatives in rats. Julian J. Ott, Mona M. Spilhaug, Simone Maschauer, Waqas Rafique, Jimmy E. Jakobsson, Karoline Hartvig, Harald Huebner, Peter Gmeiner, Olaf Prante, Patrick J. Riss. J. Med. Chem. 2020, 63, 9484-9499. [doi>10.1021/acs.jmedchem.0c00683]

298 Structure-based development of a subtype-selective orexin 1 receptor antagonist. Jan Hellmann, Matthaeus Drabek, Jie Yin, Jakub Gunera, Theresa Proell, Frank Kraus, Christopher J. Langmead, Harald Huebner, Dorothee Weikert, Peter Kolb, Daniel M. Rosenbaum, Peter Gmeiner. PNAS 2020, 117, 18059-18067. [doi>10.1073/pnas.2002704117]

297 An allosteric modulator binds to a conformational hub in the Beta2 adrenergic receptor. Xiangyu Liu, Jonas Kaindl, Magdalena Korczynska, Anne Stoessel, Daniela Dengler, Markus Stanek, Harald Huebner, Mary J. Clark, Jake Mahoney, Rachel Ann Matt, Xinyu Xu, Kunio Hirata, Brian K. Shoichet, Roger K. Sunahara, Brian K. Kobilka, Peter Gmeiner. Nat. Chem. Biol. 2020, 16, 749-755. [doi>10.1038/s41589-020-0549-2] 

296 Discovery of Novel Nonpeptidic PAR2 Ligands. Ilona Kloesel, Maximilian F. Schmidt, Jonas Kaindl, Harald Huebner, Dorothee Weikert, Peter Gmeiner. ACS Med. Chem. Lett. 2020, 11, 1316-1323. [doi>10.1021/acsmedchemlett.0c00154] 

295 Synthesis, radiosynthesis and biological evaluation of buprenorphine-derived phenylazocarboxamides as novel mu-opioid receptor ligands. Jasmin Kruell, Stefanie K. Fehler, Laura Hofmann, Natascha Nebel, Simone Maschauer, Olaf Prante, Peter Gmeiner, Harald Lanig, Harald Huebner, Markus Rolf Heinrich. ChemMedChem 2020, 15, 1175-1186. [doi>10.1002/cmdc.202000180] 

294 Regiospecific introduction of halogens on the 2-aminobiphenyl subunit leads to highly potent and selective M3 muscarinic acetylcholine receptor antagonists and weak inverse agonists. Oliver Fischer, Josefa Hofmann, Hannelore Rampp, Jonas Kaindl, Gerald Pratsch, Amelie Bartuschat, Regina Verena Taudte, Martin Friedrich Fromm, Harald Huebner, Peter Gmeiner, Markus Rolf Heinrich. J. Med. Chem. 2020, 63, 4349-4369. [doi>10.1021/acs.jmedchem.0c00297] 

293 Red-emitting dibenzodiazepinone derivatives as fluorescent dualsteric probes for the muscarinic acetylcholine M2 receptor. Xueke She, Andrea Pegoli, Corinna G. Gruber, David Wifling, Jessica Carpenter, Harald Huebner, Mengya Chen, Jianfei Wan, Guenther Bernhardt, Peter Gmeiner, Nicholas D. Holliday, Max Keller. J. Med. Chem. 2020, 63, 4133-4154. [doi>10.1021/acs.jmedchem.9b02172] 

292 Investigation of inactive state kappa opioid receptor homodimerization via single molecule microscopy using new antagonistic fluorescent probes. Antonios Drakopoulos, Zsombor Koszegi, Yann Lanoiselee, Harald Huebner, Peter Gmeiner, Davide Calebiro, Michael Decker. J. Med. Chem. 2020, 63, 3596-3609. [doi>10.1021/acs.jmedchem.9b02011] 

291 Activation of the Alpha2B adrenoceptor by the sedative sympatholytic dexmedetomidine. Daopeng Yuan, Zhongmin Liu, Jonas Kaindl, Shoji Maeda, Jiawei Zhao, Xiaoou Sun, Jun Xu, Peter Gmeiner, Hong-Wei Wang, Brian K. Kobilka. Nat. Chem. Biol. 2020, 16, 507-512. [doi>10.1038/s41589-020-0492-2]

290 Stepwise Dosing Protocol for Increased Throughput in Label-Free Impedance-Based GPCR Assays. Judith A. Stolwijk, Anne-Kathrin Mildner, Christian Kade, Michael Skiba, Guenther Bernhardt, Armin Buschauer, Harald Huebner, Peter Gmeiner, Joachim Wegener. J. Vis. Exp. 2020. [doi>10.3791/60686] 

289 Structure-based development of caged dopamine D2/D3 receptor antagonists. Marie Gienger, Harald Huebner, Stefan Loeber, Burkhard Koenig, Peter Gmeiner. Sci. Rep. 2020, 10, 829. [doi>10.1038/s41598-020-57770-9]

288 Selective and Wash-Resistant Fluorescent Dihydrocodeinone-Derivatives Allow Single-Molecule Imaging of mu-Opioid Receptor Dimerisation. Christian Gentzsch, Kerstin Seier, Antonios Drakopoulos, Marie-Lise Jobin, Yann Lanoiselee, Zsombor Koszegi, Damien Maurel, Remy Sounier, Harald Huebner, Peter Gmeiner, Sebastien Granier, Davide Calebiro, Michael Decker. Ang. Chem. 2020, 132, 2-9. [doi>10.1002/ange.201912683] Ang. Chem. Int. Ed. 2020, 59, 2-9. [doi>10.1002/anie.201912683] Supp. Info

287 Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity. Max Keller, Shahani A. Mahuroof, Vivyanne Hong Yee, Jessica Carpenter, Lisa Schindler, Timo Littmann, Andrea Pegoli, Harald Huebner, Guenther Bernhardt, Peter Gmeiner, Nicholas D. Holliday. ACS Med. Chem. Lett. 2020, 11, 16-22. [doi>10.1021/acsmedchemlett.9b00462] 

286 Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back. Antonella Di Pizio, Lukas A. W. Waterloo, Regine Brox, Stefan Loeber, Dorothee Weikert, Maik Behrens, Peter Gmeiner, Masha Y. Niv. Cell. Mol. Life Sci. 2020, 77, 531-542. [doi>10.1007/s00018-019-03194-2]

2019

285 Beta-Adrenergic Receptor Allosteric Modulators. Brian K. Kobilka, Cheng Zhang, Xiangyu Liu, Peter Gmeiner, Anne Stoessel, Harald Huebner, Daniela Dengler, Markus Stanek, Brian S. Shoichet, Magdalena Korczynska, Jacob P. Mahoney, Jonas Kaindl. WO 2019/204768 A1 20191024, PCT Int. Appl. (2019). 

284 Differential allosteric modulation within dopamine D2R – neurotensin NTS1R and D2R – serotonin 5-HT2AR receptor complexes gives bias to intracellular calcium signalling. Michael Plach, Thorsten Schaefer, Dasiel Oscar Borroto-Escuela, Dorothee Weikert, Peter Gmeiner, Kjell Fuxe, Kristina Friedland. Sci. Rep. 2019, 9, 16312. [doi>10.1038/s41598-019-52540-8] 

283 Benzyl phenylsemicarbazides: a chemistry-driven approach leading to G protein-biased dopamine D4 receptor agonists with high subtype selectivity. Anna Pirzer, Roman Lasch, Heike Friedrich, Harald Huebner, Peter Gmeiner, Markus Rolf Heinrich. J. Med. Chem. 2019, 62, 9658-9679. [doi>10.1021/acs.jmedchem.9b01085] 

282 Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. Matthias Scheiner, Dominik Dolles, Sandra Gunesch, Matthias Hoffmann, Massimo Nabissi, Oliviero Marinelli, Marina Naldi, Manuela Bartolini, Sabrina Petralla, Eleonora Poeta, Barbara Monti, Christina Falkeis, Michael Vieth, Harald Huebner, Peter Gmeiner, Rangan Maitra, Tangui Maurice, Michael Decker. J. Med. Chem. 2019, 62, 9078-9102. [doi>10.1021/acs.jmedchem.9b00623] 

281 Perquinolines A-C: Unprecedented Bacterial Tetrahydroisoquinolines Involving an Intriguing Biosynthesis. Yuriy Rebets, Suvd Nadmid, Constanze Paulus, Charlotte Dahlem, Jennifer Herrmann, Harald Huebner, Christian Rueckert, Alexandra K. Kiemer, Peter Gmeiner, Joern Kalinowski, Rolf Mueller, Andriy Luzhetskyy. Angew. Chem. 2019, 131, 13063-13068. [doi>10.1002/ange.201905538] internal link Angew. Chem. Int. Ed. 2019, 58, 12930-12934. [doi>10.1002/anie.201905538]  Supp. Info

280 Preparation of fluorophenyl substituted muscarinic receptor ligands with selectivity for M3 over M2. Ashutosh Banerjee, Amelie Bartuschat, Katrin Eitel, Peter Gmeiner, Markus Heinrich, Josefa Hofmann, Harald Huebner, Hannelore Rampp, Benjamin Schaake, Brian Kobilka, Roger Sunahara, Mary J. Clark, Inbar Fish, Brian Shoichet. WO 2019110521 A1 20190613, PCT Int. Appl. (2019). 

279 Preparation of 1,2,3,4-tetrahydronaphthalen-1-ol compounds as beta-2 selective adrenergic receptor agonists for treatment of bronchoconstrictive and cardiovascular diseases. Roger Sunahara, Harald Huebner, Jeremy Shonberg, Anne Stoessel, Markus Stanek, Dorothee Moeller, Mary Joyce Clark, Brian K. Kobilka, Peter Gmeiner, Luis Maul. WO 2019112913 A1 20190613, PCT Int. Appl. (2019). 

278 Development of covalent antagonists for beta1- and beta2-adrenergic receptors. Tobias Schwalbe, Harald Huebner, Peter Gmeiner. Bioorg. Med. Chem. 2019, 27, 2959-2971. [doi>10.1016/j.bmc.2019.05.034] 

277 Conformational Complexity and Dynamics in a Muscarinic Receptor Revealed by NMR Spectroscopy. Jun Xu, Yunfei Hu, Jonas Kaindl, Philipp Risel, Harald Huebner, Shoji Maeda, Xiaogang Niu, Hongwei Li, Peter Gmeiner, Changwen Jin, Brian K. Kobilka. Mol. Cell 2019, 75, 53-65. [doi>10.1016/j.molcel.2019.04.028] 

276 Conjugation of short peptides to dibenzodiazepinone-type muscarinic acetylcholine receptor ligands determines M2R selectivity. Andrea Pegoli, David Wifling, Corinna G. Gruber, Xueke She, Harald Huebner, Guenther Bernhardt, Peter Gmeiner, Max Keller. J. Med. Chem. 2019, 62, 5358-5369. [doi>10.1021/acs.jmedchem.8b01967] 

275 Structure-based exploration of an allosteric binding pocket in the NTS1 receptor using bitopic NT(8-13) derivatives and molecular-dynamics simulations. Ralf Christian Kling, Carolin Burchardt, Juergen Einsiedel, Harald Huebner, Peter Gmeiner. J. Mol. Model. 2019, 25, 193. [doi>10.1007/s00894-019-4064-x] 

274 Hybridization of beta-adrenergic agonists and antagonists confers G protein bias. Markus Stanek, Louis-Philippe Picard, Maximilian F. Schmidt, Jonas M. Kaindl, Harald Huebner, Michel Bouvier, Dorothee Weikert, Peter Gmeiner. J. Med. Chem. 2019, 62, 5111-5131. [doi>10.1021/acs.jmedchem.9b00349] 

273 Mast Cell Degranulation and Fibroblast Activation in the Morphine-induced Spinal Mass. Tony L. Yaksh, Kelly A. Eddinger, Shinichi Kokubu, Zhenping Wang, Anna DiNardo, Roshni Ramachandran, Yuelian Zhu, Yajun He, Fieke Weren, Daphne Quang, Shelle A. Malkmus, Katherine Lansu, Wesley K. Kroeze, Brian Eliceiri, Joanne J. Steinauer, Peter W. Schiller, Peter Gmeiner, Linda M. Page, Keith R. Hildebrand. Anesthesiology 2019, 131, 132-147. [doi>10.1097/ALN.0000000000002730] educational video 

272 Increasing the throughput of label-free cell assays to study the activation of G-protein-coupled receptors by using a serial agonist exposure protocol. Judith A. Stolwijk, Michael Skiba, Christian Kade, Guenther Bernhardt, Armin Buschauer, Harald Huebner, Peter Gmeiner, Joachim Wegener. Integr. Biol. 2019, 11, 99-108. [doi>10.1093/intbio/zyz010] 

271 Synthesis of pyrazolylvinyl ketones from furan derivatives. Nattawut Sawengngen, Petrakis N. Chalikidi, Sara Araby, Frank Hampel, Peter Gmeiner, Olga V. Serdyuk. Org. Biomol. Chem. 2019, 17, 4850-4855. [doi>10.1039/c9ob00701f] 

270 Monitoring of the dopamine D2 receptor agonists hordenine and N-methyltyramine during the brewing process and in commercial beer samples. Thomas Sommer, Gelena Dlugash, Harald Huebner, Peter Gmeiner, Monika Pischetsrieder. Food Chem. 2019, 276, 745-753. [doi>10.1016/j.foodchem.2018.10.067]  Supp Info

269 Urea derivatives as mu-opioid receptor modulators and their preparation. Brian K. Shoichet, Anat Levit, Aashish Manglik, Brian Kobilka, Peter Gmeiner, Harald Huebner, Daniela Gisela Dengler. WO 2019036678 A1 20190221, PCT Int. Appl. (2019). 

2018

268 Preparation of mu-opioid receptor modulators. Brian K. Shoichet, Peter Gmeiner, Harald Huebner, Bryan L. Roth, Daniela Dengler, Aashish Manglik, Brian Kobilka. WO 2018129393 A1 20180712, PCT Int. Appl. (2018). 

267 Preparation of lutetium complex DOTA derivs. for diagnosis, treatment and prevention of neurotensin receptor-related conditions. Olaf Prante, Torsten Kuwert, Peter Gmeiner, Ashutosh Banerjee, Simone Maschauer. WO 2018024789 A1 20180208, PCT Int. Appl. (2018). 

266 Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists. Hongtao Liu, Josefa Hofmann, Inbar Fish, Benjamin Schaake, Katrin Eitel, Amelie Bartuschat, Jonas Kaindl, Hannelore Rampp, Ashutosh Banerjee, Harald Huebner, Mary J. Clark, Sandra G. Vincent, John T. Fisher, Markus R. Heinrich, Kunio Hirata, Xiangyu Liu, Roger K. Sunahara, Brian K. Shoichet, Brian K. Kobilka, and Peter Gmeiner. PNAS 2018, 115, 12046-12050. [doi>10.1073/pnas.1813988115] 

265 Derivatization of common antidepressant drugs increases inhibition of acid sphingomyelinase and reduces induction of phospholipidosis. Cosima Rhein, Stefan Loeber, Peter Gmeiner, Erich Gulbins, Philipp Tripal, Johannes Kornhuber. J. Neural Transm. 2018, 125, 1837-1845. [doi>10.1007/s00702-018-1923-z] 

2017

264 [¹⁸F]Fluorophenylazocarboxylates: Design and Synthesis of Potential Radioligands for Dopamine D3 and mu-Opioid Receptor. Natascha Nebel, Brigitte Strauch, Simone Maschauer, Roman Lasch, Hannelore Rampp, Stefanie K. Fehler, Leonard R. Bock, Harald Huebner, Peter Gmeiner, Markus R. Heinrich, Olaf Prante. ACS Omega 2017, 2, 8649-8659. [doi>10.1021/acsomega.7b01374] 

263    Structure-Based Design and Discovery of New M2 Receptor Agonists. Inbar Fish, Anne Stoessel, Katrin Eitel, Celine Valant, Sabine Albold, Harald Huebner, Dorothee Moeller, Mary J. Clark, Roger K. Sunahara, Arthur Christopoulos, Brian K. Shoichet, Peter Gmeiner. J. Med. Chem. 2017, 60, 9239-9250. [doi>10.1021/acs.jmedchem.7b01113] 

262    Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity. Xueke She, Andrea Pegoli, Judith Mayr, Harald Huebner, Guenther Bernhardt, Peter Gmeiner, Max Keller. ACS Omega 2017, 2, 6741-6754. [doi>10.1021/acsomega.7b01085] 

261    Visualization of ligand-induced dopamine D2S and D2L receptor internalization by TIRF microscopy. Alina Tabor, Dorothee Moeller, Harald Huebner, Johannes Kornhuber, Peter Gmeiner. Sci. Rep. 2017, 7, 10894. [doi>10.1038/s41598-017-11436-1] 

260    Structure-guided screening for functionally selective D2 dopamine receptor ligands from a virtual chemical library. Barbara Maennel, Mariama Jaiteh, Alexey Zeifman, Alena Randakova, Dorothee Moeller, Harald Huebner, Peter Gmeiner, Jens Carlsson. ACS Chem. Biol. 2017, 12, 2652-2661. [doi>10.1021/acschembio.7b00493] 

259    Beta-arrestin biased dopamine D2 receptor partial agonists: synthesis and pharmacological evaluation. Barbara Maennel, Harald Huebner, Dorothee Moeller, Peter Gmeiner. Bioorg. Med. Chem. 2017, 25, 5613-5628. [doi>10.1016/j.bmc.2017.08.037] Supp. Info

258    Photochromic Dopamine Receptor Ligands Based on Dithienylethenes and Fulgides. Daniel Lachmann, Carolin Studte, Barbara Maennel, Harald Huebner, Peter Gmeiner, Burkhard Koenig. Chem. Eur. J. 2017, 23, 13423-13434. [doi>10.1002/chem.201702147] 

257    Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. Tobias Schwalbe, Jonas Kaindl, Harald Huebner, Peter Gmeiner. Bioorg. Med. Chem. 2017, 25, 5084-5094. [doi>10.1016/j.bmc.2017.06.034]  Supp. Info

256    Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for Beta-Arrestin-Biased D2R Agonists. Barbara Maennel, Daniela Dengler, Jeremy Shonberg, Harald Huebner, Dorothee Moeller, Peter Gmeiner. J. Med. Chem. 2017, 60, 4693-4713. [doi>10.1021/acs.jmedchem.7b00363] 

255    Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior. Anne Stoessel, Regine Brox, Nirupam Purkayastha, Harald Huebner, Carsten Hocke, Olaf Prante, Peter Gmeiner. Bioorg. Med. Chem. 2017, 25, 3491-3499. [doi>10.1016/j.bmc.2017.04.036] Supp. Info

254    Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor. Andrea Pegoli, Xueke She, David Wifling, Harald Huebner, Guenther Bernhardt, Peter Gmeiner, Max Keller. J. Med. Chem. 2017, 60, 3314-3334. [doi>10.1021/acs.jmedchem.6b01892] 

253    Preparation of selective mu-opioid receptor modulators for treatment of pain. Bryan L. Roth, Daniela Gisela Dengler, Brian K. Shoichet, Henry Lin, Peter Gmeiner, Aashish Manglik, Brian Kobilka. WO 2017007695 A1 20170112, PCT Int. Appl. (2017). 

252    Theranostic Value of Multimers: Lessons Learned from Trimerization of Neurotensin Receptor Ligands and Other Targeting Vectors. Simone Maschauer, Juergen Einsiedel, Dominik Reich, Harald Huebner, Peter Gmeiner, Hans-Juergen Wester, Olaf Prante, Johannes Notni. Pharmaceuticals 2017, 10, 29. [doi>10.3390/ph10010029] 

251    Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. Dorothee Moeller, Ashutosh Banerjee, Taygun C. Uzuneser, Marika Skultety, Tobias Huth, Bianca Plouffe, Harald Huebner, Christian Alzheimer, Kristina Friedland, Christian P. Mueller, Michel Bouvier, Peter Gmeiner. J. Med. Chem. 2017, 60, 2908-2929. [doi>10.1021/acs.jmedchem.6b01857] 

250    Identification of the Beer Component Hordenine as Food-Derived Dopamine D2 Receptor Agonist by Virtual Screening a 3D Compound Database. Thomas Sommer, Harald Huebner, Ahmed El Kerdawy, Peter Gmeiner, Monika Pischetsrieder, Timothy Clark. Scientific Reports 2017, 7, 44201. [doi>10.1038/srep44201] 

249    NTS2-Selective Neurotensin Mimetics with Tetrahydrofuran Amino Acids. Nadja A. Simeth, Manuel Bause, Michael Dobmeier, Ralf C. Kling, Daniel Lachmann, Harald Huebner, Juergen Einsiedel, Peter Gmeiner, Burkhard Koenig. Bioorg. Med. Chem. 2017, 25, 350-359. [doi>10.1016/j.bmc.2016.10.039] Supp. Info

2016

248    Dibenzo[b,f][1,4]oxazepines and dibenzo[b,e]oxepines: Influence of the chlorine substitution pattern on the pharmacology at the H1R, H4R, 5-HT2AR and other selected GPCRs. Franziska Naporra, Susanne Gobleder, Hans-Joachim Wittmann, Julia Spindler, Michael Bodensteiner, Guenther Bernhardt, Harald Huebner, Peter Gmeiner, Sigurd Elz, Andrea Strasser. Pharmacol. Res. 2016, 113, 610-625. [doi>10.1016/j.phrs.2016.09.042]  Supp. Info

247    Visualization and ligand-induced modulation of dopamine receptor dimerization at the single molecule level. Alina Tabor, Siegfried Weisenburger, Ashutosh Banerjee, Nirupam Purkayastha, Jonas M. Kaindl, Harald Huebner, Luxi Wei, Teja W. Groemer, Johannes Kornhuber, Nuska Tschammer, Nigel J. M. Birdsall, Gregory I. Mashanov, Vahid Sandoghdar, Peter Gmeiner. Sci. Rep. 2016, 6, 33233. [doi>10.1038/srep33233] 

246    Structure-based discovery of opioid analgesics with reduced side effects. Aashish Manglik, Henry Lin, Dipendra K. Aryal, John D. McCorvy, Daniela Dengler, Gregory Corder, Anat Levit, Ralf C. Kling, Viachaslau Bernat, Harald Huebner, Xi-Ping Huang, Maria F. Sassano, Patrick M. Giguere, Stefan Loeber, Da Duan, Gregory Scherrer, Brian K. Kobilka, Peter Gmeiner, Bryan L. Roth, Brian K. Shoichet. Nature 2016, 537, 185-190. [doi>10.1038/nature19112] 

245    Structure-guided development of heterodimer-selective GPCR ligands. Harald Huebner, Tamara Schellhorn, Marie Gienger, Carolin Schaab, Jonas Kaindl, Laurin Leeb, Timothy Clark, Dorothee Moeller, and Peter Gmeiner. Nat. Commun. 2016, 7, 12298. [doi>10.1038/ncomms12298] 

244    ¹⁸F- and ⁶⁸Ga-labeled Neurotensin Peptides for PET Imaging of Neurotensin Receptor 1. Simone Maschauer, Juergen Einsiedel, Harald Huebner, Peter Gmeiner, and Olaf Prante. J. Med. Chem. 2016, 59, 6480-6492. [doi>10.1021/acs.jmedchem.6b00675] 

243    Spontaneous butenolide ring formation of pregnane-21-O-malonyl hemiesters under mild reaction conditions is facilitated by the 14beta-hydroxy group present in all natural cardenolides. R.M. Padua, , N. Meitinger, M. Hennemann, P. Schebitz, R. Waibel, S. Loeber, P. Gmeiner, T. Clark, W. Kreis. Tetrahedron 2016, 72, 4556-4563. [doi>10.1016/j.tet.2016.06.024] 

242    Structure-guided development of dual Beta 2 adrenergic/dopamine D2 receptor agonists. Dietmar Weichert, Markus Stanek, Harald Huebner, Peter Gmeiner. Bioorg. Med. Chem. 2016, 24, 2641-2653. [doi>10.1016/j.bmc.2016.04.028]  Supp. Info

241    Mimicking of Arginine by Functionalized N omega-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples. Max Keller, Kilian K. Kuhn, Juergen Einsiedel, Harald Huebner, Sabrina Biselli, Catherine Mollereau, David Wifling, Jaroslava Svobodova, Guenther Bernhardt, Chiara Cabrele, Patrick M. L. Vanderheyden, Peter Gmeiner, and Armin Buschauer. J. Med. Chem. 2016, 59, 1925-1945. [doi>10.1021/acs.jmedchem.5b01495] 

240    Development of Covalent Ligand-Receptor Pairs to Study the Binding Properties of Nonpeptidic Neurotensin Receptor 1 Antagonists. Ralf C. Kling, Manuel Plomer, Christopher Lang, Ashutosh Banerjee, Harald Huebner, and Peter Gmeiner. ACS Chem. Biol. 2016, 11, 869-875. [doi>10.1021/acschembio.5b00965] 

239    Optimization and synthesis of an 18F-labeled dopamine D3 receptor ligand using [¹⁸F]fluorophenylazocarboxylic tert-butylester. Natascha Nebel, Simone Maschauer, Carsten Hocke, Harald Huebner, Peter Gmeiner and Olaf Prante. J. Label Compd. Radiopharm 2016, 59, 48-53. [doi>10.1002/jlcr.3361] 

238    Comparative MD Simulations Indicate a Dual Role for Arg1323.50 in Dopamine-Dependent D2R Activation. Ralf C. Kling, Timothy Clark, Peter Gmeiner. PLOS ONE 2016, 11, e0146612. [doi>10.1371/journal.pone.0146612]

2015

237    The broad-spectrum antiinfective drug artesunate interferes with the canonical nuclear factor kappa B (NF-kB) pathway by targeting RelA/p65. Corina Hutterer, Ina Niemann, Jens Milbradt, Tony Froehlich, Christoph Reiter, Onat Kadioglu, Hanife Bahsi, Isabel Zeittraeger, Sabrina Wagner, Juergen Einsiedel, Peter Gmeiner, Nico Vogel, Sebastian Wandinger, Klaus Godl, Thomas Stamminger, Thomas Efferth, Svetlana B. Tsogoeva, Manfred Marschall. Antiviral Res. 2015, 124, 101-109. [doi>10.1016/j.antiviral.2015.10.003] Supp Info

236    Arrestin-Bound Rhodopsin: A Molecular Structure and its Impact on the Development of Biased GPCR Ligands. Dorothee Moeller, Peter Gmeiner. Angew. Chem. Int. Ed. 2015, 54, 13166-13168. [doi>10.1002/anie.201507724]  Die Rhodopsin-Arrestin-Kristallstruktur und ihre Bedeutung fuer die Entwicklung funktionell selektiver GPCR-Wirkstoffe. Dorothee Moeller, Peter Gmeiner. Angew. Chem. 2015, 127, 13362-13364. [doi>10.1002/ange.201507724] 

235    Structural insights into mu-opioid receptor activation. Weijiao Huang, Aashish Manglik, A. J. Venkatakrishnan, Toon Laeremans, Evan N. Feinberg, Adrian L. Sanborn, Hideaki E. Kato, Kathryn E. Livingston, Thor S. Thorsen, Ralf C. Kling, Sebastien Granier, Peter Gmeiner, Stephen M. Husbands, John R. Traynor, William I. Weis, Jan Steyaert, Ron O. Dror, Brian K. Kobilka. Nature 2015, 524, 315-321. [doi>10.1038/nature14886] 

234    1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: quantitative structure selectivity investigations, docking, synthesis and biological evaluation. Dorothee Moeller, Ismail Salama, Ralf C. Kling, Harald Huebner, Peter Gmeiner. Bioorg. Med. Chem. 2015, 23, 6195-6209. [doi>10.1016/j.bmc.2015.07.050] 

233    Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library. Mattia Stucchi, Peter Gmeiner, Harald Huebner, Giulia Rainoldi, Alessandro Sacchetti, Alessandra Silvani, and Giordano Lesma, ACS Med. Chem. Lett. 2015, 6, 882-887. [doi>10.1021/acsmedchemlett.5b00131] 

232    Covalent molecular probes for class A G protein-coupled receptors: advances and applications. Dietmar Weichert and Peter Gmeiner, ACS Chem. Biol. 2015, 10, 1376-1386. [doi>10.1021/acschembio.5b00070] 

231    Selective GPCR ligands. Peter Gmeiner, Bioorg. Med. Chem. 2015, 23, 3879. [doi>10.1016/j.bmc.2015.03.030] 

230    Molecular Determinants of Biased Agonism at the Dopamine D2 Receptor. Dietmar Weichert, Ashutosh Banerjee, Christine Hiller, Ralf C. Kling, Harald Huebner, and Peter Gmeiner, J. Med. Chem. 2015, 58, 2703-2717. [doi>10.1021/jm501889t] 

229    Improved radiosynthesis and preliminary in vivo evaluation of a ¹⁸F-labeled glycopeptide-peptoid hybrid for PET imaging of neurotensin receptor 2. Simone Maschauer, Cornelia Greff, Juergen Einsiedel, Julian Ott, Philipp Tripal, Harald Huebner, Peter Gmeiner, and Olaf Prante, Bioorg. Med. Chem. 2015, 23, 4026-4033. [doi>10.1016/j.bmc.2015.01.053] Supp. Info

228    GPCR crystal structures: Medicinal chemistry in the pocket. Jeremy Shonberg, Ralf C. Kling, Peter Gmeiner, and Stefan Loeber, Bioorg. Med. Chem. 2015, 23, 3880-3906. [doi>10.1016/j.bmc.2014.12.034] 

227    Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. Amelie L. Bartuschat, Tamara Schellhorn, Harald Huebner, Peter Gmeiner, and Markus R. Heinrich, Bioorg. Med. Chem. 2015, 23, 3938-3947. [doi>10.1016/j.bmc.2014.12.012] 

2014

226    Structure-Based Evolution of Subtype-Selective Neurotensin Receptor Ligands. Carolin Schaab, Ralf Christian Kling, Juergen Einsiedel, Harald Huebner, Tim Clark, Dieter Seebach, and Peter Gmeiner, ChemistryOpen 2014, 3, 206-218. [doi>10.1002/open.201402031]

225    Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging. Natascha Nebel, Simone Maschauer, Amelie L. Bartuschat, Stefanie K. Fehler, Harald Huebner, Peter Gmeiner, Torsten Kuwert, Markus R. Heinrich, Olaf Prante, Carsten Hocke, Bioorg. Med. Chem. Lett. 2014, 24, 5399-5403. [doi>10.1016/j.bmcl.2014.10.043]

224    H-CRRETAWAC-OH, a Lead Structure for the Development of Radiotracer Targeting Integrin Alpha5Beta1? Roland Haubner, Simone Maschauer, Juergen Einsiedel, Iris E. Eder, Christine Rangger, Peter Gmeiner, Irene J. Virgolini, and Olaf Prante, BioMed Research International 2014, Article ID 243185. [doi>10.1155/2014/243185]

223    Covalent agonists for studying G protein-coupled receptor activation. Dietmar Weichert, Andrew C. Kruse, Aashish Manglik, Christine Hiller, Cheng Zhang, Harald Huebner, Brian K. Kobilka, and Peter Gmeiner, Proc. Natl. Acad. Sci. USA 2014, 111, 10744-10748. [doi>10.1073/pnas.1410415111]

222    Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D2-like receptors. Ismail Salama, Stefan Loeber, Harald Huebner, Peter Gmeiner, Bioorg. Med. Chem. Lett. 2014, 24, 3753-3756. [doi>10.1016/j.bmcl.2014.06.079]

221    Functionally Selective Dopamine D2, D3 Receptor Partial Agonists. Dorothee Moeller, Ralf C. Kling, Marika Skultety, Kristina Leuner, Harald Huebner, and Peter Gmeiner, J. Med. Chem. 2014, 57, 4861-4875. [doi>10.1021/jm5004039]

220    Active-State Model of a Dopamine D2 Receptor – Galphai Complex Stabilized by Aripiprazole-Type Partial Agonists. Ralf C. Kling, Nuska Tschammer, Harald Lanig, Timothy Clark, Peter Gmeiner, PLOS ONE 2014, 9, e100069. [doi>10.1371/journal.pone.0100069]

219    GPCRs as highly relevant targets for the development of efficient drugs. Christine Hiller and Peter Gmeiner, BIOspektrum 2014, 20, 15-18. [doi>10.1007/s12268-014-0398-1]

218    In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study. Simone Maschauer, Tina Ruckdeschel, Philipp Tripal, Roland Haubner, Juergen Einsiedel, Harald Huebner, Peter Gmeiner, Torsten Kuwert and Olaf Prante, Pharmaceuticals 2014, 7, 464-481. [doi>10.3390/ph7040464]

217    Biodistribution studies of two ¹⁸F-labeled pyridinylphenyl amides as subtype selective radioligands for the dopamine D3 receptor. Carsten Hocke, Paul Cumming, Simone Maschauer, Torsten Kuwert, Peter Gmeiner, Olaf Prante, Nuclear Medicine and Biology 2014, 41, 223-228. [doi>10.1016/j.nucmedbio.2013.12.014]

216    Fast and efficient ¹⁸F-labeling via [18F]fluorophenylazocarboxylic esters. Stefanie K. Fehler, Simone Maschauer, Sarah B. Hoefling, Amelie L. Bartuschat, Nuska Tschammer, Harald Huebner, Peter Gmeiner, Olaf Prante, Markus R. Heinrich, Chem. Eur. J. 2014, 20, 370-375. [doi>10.1002/chem.201303409]

2013

215    Activation and allosteric modulation of a muscarinic acetylcholine receptor. Andrew C. Kruse, Aaron M. Ring, Aashish Manglik, Jianxin Hu, Kelly Hu, Katrin Eitel, Harald Huebner, Els Pardon, Celine Valant, Patrick M. Sexton, Arthur Christopoulos, Christian C. Felder, Peter Gmeiner, Jan Steyaert, William I. Weis, K. Christopher Garcia, Juergen Wess, and Brian K. Kobilka, Nature 2013, 504, 101-106. [doi>10.1038/nature12735]

214    Synthesis and Evaluation of a ¹⁸F-Labeled Diarylpyrazole Glycoconjugate for the Imaging of NTS1 positive tumors. Christopher Lang, Simone Maschauer, Harald Huebner, Peter Gmeiner, and Olaf Prante, J. Med. Chem. 2013, 56, 9361-9365. [doi>10.1021/jm401491e]

213    Syntheses, Receptor Bindings, in vitro and in vivo Stabilities and Biodistributions of DOTA-Neurotensin(8-13) Derivatives Containing Beta-Amino Acid Residues – A Lesson about the Importance of Animal Experiments. Christof Sparr, Nirupam Purkayastha, Tomohiro Yoshinari, Dieter Seebach, Simone Maschauer, Olaf Prante, Harald Huebner, Peter Gmeiner, Beata Kolesinska, Renzo Cescato, Beatrice Waser, and Jean Claude Reubi, Chemistry & Biodiversity 2013, 10, 2101-2121. pdf

212    Struktur und Funktion beta-adrenerger Rezeptoren. Cornelia Held, Ralf Kling, Peter Gmeiner, Pharmakon 2013, 1, 406-412. pdf

211    Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers. Ashutosh Banerjee, Simone Maschauer, Harald Huebner, Peter Gmeiner, Olaf Prante, Bioorg. Med. Chem. Lett. 2013, 23, 6079-6082. [doi>10.1016/j.bmcl.2013.09.026]

210    Muscarinic receptors as model targets and antitargets for structure-based ligand discovery. Andrew C. Kruse, Dahlia R. Weiss, Mario Rossi, Jianxin Hu, Kelly Hu, Katrin Eitel, Peter Gmeiner, Juergen Wess, Brian K. Kobilka, and Brian K. Shoichet, Mol. Pharmacol. 2013, 84, 528-540. [doi>10.1124/mol.113.087551]

209    Pharmacological Profile of 2-Bromoterguride at Human Dopamine D2, Porcine Serotonin 5-HT2A and Alpha2C-Adrenergic Receptors, and its Antipsychotic-Like Effects in Rats. Florian Jantschak, Jan Brosda, Robert T. Franke, Heidrun Fink, Dorothee Moeller, Harald Huebner, Peter Gmeiner, and Heinz H. Pertz, JPET 2013, 347, 57-68. [doi>10.1124/jpet.113.205997]

208    Argyreia nervosa (Burm. f.): Receptor profiling of lysergic acid amide and other potential psychedelic LSD-like compounds by computational and binding assay approaches. Alexander Paulke, Christian Kremer, Cora Wunder, Janosch Achenbach, Bardya Djahanschiri, Anderson Elias, J. Stefan Schwed, Harald Huebner, Peter Gmeiner, Ewgenij Proschak, Stefan W. Toennes, Holger Stark, Journal of Ethnopharmacology 2013, 148, 492-497. [doi>10.1016/j.jep.2013.04.044]

207    Functionally Selective Dopamine D2/D3 Receptor Agonists Comprising an Enyne Moiety. Christine Hiller, Ralf C. Kling, Frank W. Heinemann, Karsten Meyer, Harald Huebner, and Peter Gmeiner, J. Med. Chem. 2013, 56, 5130-5141. [doi>10.1021/jm400520c]

206    Active-state models of ternary GPCR complexes: Determinants of selective receptor-G-protein coupling. Ralf C. Kling, Harald Lanig, Timothy Clark, and Peter Gmeiner, PLOS ONE 2013, 8, e67244. [doi>10.1371/journal.pone.0067244]

205    Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation. Christopher Lang und Peter Gmeiner, Synthesis 2013, 45, 2474-2480. [doi>10.1055/s-0033-1338497]

204    Class A G protein-coupled receptor (GPCR) dimers and bivalent ligands. Christine Hiller, Julia Kuehhorn, and Peter Gmeiner, J. Med. Chem. 2013, 56, 6542-6559. [doi>10.1021/jm4004335]

203    Dopamine agonist-induced penile erection and yawning: A comparative study in outbred Roman high- and low-avoidance rats. Fabrizio Sanna, Maria Giuseppa Corda, Maria Rosaria Melis, Maria Antonietta Piludu, Stefan Loeber, Harald Huebner, Peter Gmeiner, Antonio Argiolas, Osvaldo Giorgi, Pharmacology, Biochemistry and Behavior 2013, 109, 59-66. [doi>10.1016/j.pbb.2013.05.002]

202    Impact of the Proline Residue on Ligand Binding of Neurotensin Receptor 2 (NTS2)-Selective Peptide-Peptoid Hybrids. Cornelia Held, Harald Huebner, Ralf Kling, Yvonne A. Nagel, Helma Wennemers, Peter Gmeiner, ChemMedChem 2013, 8, 772-778. [doi>10.1002/cmdc.201300054]

201    The pH Probe CypHer^TM5E is Effectively Quenched by FM Dyes. Oliver Welzel, Kristina Loy, Carsten H. Tischbirek, Alina Tabor, Peter Gmeiner, Johannes Kornhuber, Teja Wolfgang Groemer, J. Fluoresc. 2013, 23, 487-494. [doi>10.1007/s10895-013-1164-3]

200    Discovery of dopamine D4 receptor antagonists with planar chirality. Fabrizio Sanna, Birgit Ortner, Harald Huebner, Stefan Loeber, Nuska Tschammer, Peter Gmeiner, Bioorg. Med. Chem. 2013, 21, 1680-1684. [doi>10.1016/j.bmc.2013.01.065]

199    Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand. Cornelia Held, Manuel Plomer, Harald Huebner, Jasmin Meltretter, Monika Pischetsrieder, and Peter Gmeiner, ChemMedChem 2013, 8, 75-81. [doi>10.1002/cmdc.201200376]

2012

198    Novel Azulene Derivatives for the Treatment of Erectile Dysfunction. Stefan Loeber, Harald Huebner, Armin Buschauer, Fabrizio Sanna, Antonio Argiolas, Maria Rosaria Melis and Peter Gmeiner, Bioorg. Med. Chem. Lett. 2012, 22, 7151-7154. [doi>10.1016/j.bmcl.2012.09.064]

197    Conformationally Restricted Peptide Mimetics by Ring-Closing Olefin Metathesis. Satish Wakchaure, Juergen Einsiedel, Reiner Waibel, Peter Gmeiner, Synthesis 2012, 44, 2682-2694. [doi>10.1055/s-0032-1316758]

196    Biotransformation of 21-O-acetyl-deoxycorticosterone by cell suspension cultures of Digitalis lanata (strain W.1.4). Rodrigo Maia de Padua, Nadine Meitinger, Jose Dias de Souza Filho, Reiner Waibel, Peter Gmeiner, Fernao Castro Braga, Wolfgang Kreis, Steroids 2012, 77, 1373-1380. [doi>10.1016/j.steroids.2012.07.016]

195    A new D2 dopamine receptor agonist allosterically modulates A2A adenosine receptor signalling by interacting with the A2A/D2 receptor heteromer. Maria Letizia Trincavelli, Simona Daniele, Elisabetta Orlandini, Gemma Navarro, Vicent Casado, Chiara Giacomelli, Susanna Nencetti, Elisa Nuti, Marco Macchia, Harald Huebner, Peter Gmeiner, Armando Rossello, Carmen LLuis, Claudia Martini, Cellular Signalling 2012, 24, 951-960. [doi>10.1016/j.cellsig.2011.12.018]

194    Selective Agonists for Dopamine/Neurotensin Receptor Heterodimers. Susanne Koschatzky, Peter Gmeiner, ChemMedChem 2012, 7, 509-514. [doi>10.1002/cmdc.201100499]

193    Bivalent molecular probes for dopamine D2-like receptors. Daniela Huber, Stefan Loeber, Harald Huebner, Peter Gmeiner, Bioorg. Med. Chem. 2012, 20, 455-466. [doi>10.1016/j.bmc.2011.10.063]

2011

192    Evaluation of ¹⁸F-labeled Benzodioxine Piperazine-based Dopamine D4 Receptor Ligands: Lipophilicity as a Determinate of Non-specific Binding. Fabian Kuegler, Wiebke Sihver, Johannes Ermert, Harald Huebner, Peter Gmeiner, Olaf Prante, Heinz H. Coenen, J. Med. Chem. 2011, 54, 8343-8352. [doi>10.1021/jm200762g]

191    Molecular Dynamics Simulations of the Effect of the G-Protein and Diffusible Ligands on the Beta2-Adrenergic Receptor. Angela Goetz, Harald Lanig, Peter Gmeiner, Timothy Clark, J. Mol. Biol. 2011, 414, 611-623. [doi>10.1016/j.jmb.2011.10.015]

190    Development of a Bivalent Dopamine D2 Receptor Agonist. Julia Kuehhorn, Angela Goetz, Harald Huebner, Dawn Thompson, Jennifer Whistler, Peter Gmeiner, J. Med. Chem. 2011, 54, 7911-7919. [doi>10.1021/jm2009919]

189    Dopamine D2-like receptor agonists induce penile erection in male rats: Differential role of D2, D3 and D4 receptors in the paraventricular nucleus of the hypothalamus. Fabrizio Sanna, Salvatora Succu, Harald Huebner, Peter Gmeiner, Antonio Argiolas, Maria Rosaria Melis, Behav. Brain Res. 2011, 225, 169-176. [doi>10.1016/j.bbr.2011.07.018]

188    New aminotetraline derivatives. Peter Gmeiner, Miriam Ruberg, Harald Huebner. WO2011076708 (2011). pdf

187    Quinpramine Ameliorates Rat Experimental Autoimmune Neuritis and Redistributes MHC Class II Molecules. Gerd Meyer zu Hoerste, Anne K. Mausberg, Johanna I. Mueller, Helmar C. Lehmann, Stefan Loeber, Peter Gmeiner, Hans-Peter Hartung, Olaf Stueve, Carsten Korth, Bernd C. Kieseier, PLoS ONE 2011, 6, e21223. pdf

186    A Highly Efficient Type I Beta-Turn Mimetic Simulating an Asx-Pro-Turn-Like Structure. Andrea Pinsker, Juergen Einsiedel, Steffen Haerterich, Reiner Waibel, and Peter Gmeiner, Org. Lett. 2011, 13, 3502-3505. [doi>10.1021/ol201313q]

185    Bivalent Dopamine D2 Receptor Ligands: Synthesis and Binding Properties. Julia Kuehhorn, Harald Huebner, and Peter Gmeiner, J. Med. Chem. 2011, 54, 4896-4903. [doi>10.1021/jm2004859]

184    On the Terminal Homologation of Physiologically Active Peptides as a Means of Increasing Stability in Human Serum – Neurotensin, Opiorphin, B27-KK10 Epitope, NPY. Dieter Seebach, Aneta Lukaszuk, Krystyna Patora-Komisarska, Dominika Podwysocka, James Gardiner, Marc-Olivier Ebert, Jean Claude Reubi, Renzo Cescato, Beatrice Waser, Peter Gmeiner, Harald Huebner, Catherine Rougeot, Chem. Biodivers. 2011, 8, 711-739. [doi>10.1002/cbdv.201100093]

183    The bulky N(6) substituent of cabergoline is responsible for agonism of this drug at serotonin 5-HT2a and 5-HT2b receptors and thus a determinant of valvular heart disease. Alexandra Kekewska, Harald Huebner, Peter Gmeiner, and Heinz H. Pertz, JPET 2011, 338, 381-391. [doi>10.1124/jpet.111.181255]

182    Cross-Receptor Interactions between Dopamine D2L and Neurotensin NTS1 Receptors Modulate Binding Affinities of Dopaminergics. Susanne Koschatzky, Nuska Tschammer, and Peter Gmeiner, ACS Chem. Neurosci. 2011, 2, 308-316. [doi>10.1021/cn200020y]

181    Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand. Gerald Pratsch, Johannes F. Unfried, Juergen Einsiedel, Manuel Plomer, Harald Huebner, Peter Gmeiner and Markus R. Heinrich, Org. Biomol. Chem. 2011, 9, 3746-3752. [doi>10.1039/c1ob05292f]

180    Discovery of Highly Potent and Neurotensin Receptor 2 Selective Neurotensin Mimetics. Juergen Einsiedel, Cornelia Held, Maud Hervet, Manuel Plomer, Nuska Tschammer, Harald Huebner, Peter Gmeiner, J. Med. Chem. 2011, 54, 2915-2923. [doi>10.1021/jm200006c]

179    Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Stefan Loeber, Harald Huebner, Nuska Tschammer, Peter Gmeiner, Trends Pharmacol. Sci. 2011, 32, 148-157. [doi>10.1016/j.tips.2010.12.003]

178    Highly Potent 5-Aminotetrahydropyrazolopyridines: Enantioselective Dopamine D3 Receptor Binding, Functional Selectivity, and Analysis of Receptor-Ligand Interactions. Nuska Tschammer, Jan Elsner, Angela Goetz, Katharina Ehrlich, Stefan Schuster, Miriam Ruberg, Julia Kuehhorn, Dawn Thompson, Jennifer Whistler, Harald Huebner, Peter Gmeiner, J. Med. Chem. 2011, 54, 2477-2491. [doi>10.1021/jm101639t]

177    Aromatic ring functionalization of benzolactam derivatives: New potent dopamine D3 receptor ligands. Raquel Ortega, Harald Huebner, Peter Gmeiner, Christian F. Masaguer, Bioorg. Med. Chem. Lett. 2011, 21, 2670-2674. [doi>10.1016/j.bmcl.2010.12.083]

176    Histidine 6.55 is a major determinant of ligand-based signaling in dopamine D2L receptor. Nuska Tschammer, Stefan Bollinger, Terry Kenakin, Peter Gmeiner, Mol. Pharmacol. 2011, 79, 575-585. [doi>10.1124/mol.110.068106]

175    Structure and function of an irreversible agonist-beta2 adrenoceptor complex. Daniel M. Rosenbaum, Cheng Zhang, Joseph A. Lyons, Ralph Holl, David Aragao, Daniel H. Arlow, Soren G.F. Rasmussen, Hee-Jung Choi, Brian T. DeVree, Roger K. Sunahara, Pil Seok Chae, Samuel H. Gellman, Ron O. Dror, David E. Shaw, William I. Weis, Martin Caffrey, Peter Gmeiner, Brian K. Kobilka, Nature 2011, 469, 236-240. [doi>10.1038/nature09665]

2010

174    Synthesis, biological evaluation and radiolabelling by ¹⁸F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET. Sarah B. Hoefling, Simone Maschauer, Harald Huebner, Peter Gmeiner, Hans-Juergen Wester, Olaf Prante, Markus R. Heinrich, Bioorg. Med. Chem. Lett. 2010, 20, 6933-6937. [doi>10.1016/j.bmcl.2010.09.142]

173    Bioisosteric Replacement Leading to Biologically Active [2.2]Paracyclophanes with Altered Binding Profiles for Aminergic G-Protein-Coupled Receptors. Marika Skultety, Harald Huebner, Stefan Loeber, Peter Gmeiner, J. Med. Chem. 2010, 53, 7219-7228. [doi>10.1021/jm100899z]

172    Novel Pyridylmethylamines as Highly Selective 5-HT1A Superagonists. Stefan Bollinger, Harald Huebner, Frank W. Heinemann, Karsten Meyer, Peter Gmeiner, J. Med. Chem. 2010, 53, 7167-7179. [doi>10.1021/jm100835q]

171    Anhydrotetracycline-Peptide Conjugates as Representatives for Ligand-Based Transactivating Systems. Susanne Lochner, Juergen Einsiedel, Gesa Schaefer, Christian Berens, Wolfgang Hillen, Peter Gmeiner, Bioorg. Med. Chem. 2010, 18, 6127-6133. [doi>10.1016/j.bmc.2010.06.061]

170    The Therapeutically Anti-prion Active Antibody-fragment scF-W226: Paramagnetic Relaxation-Enhanced NMR Spectroscopy Aided Structure Elucidation of the Paratope-epitope Interface. Christian Mangels, Ruth Kellner, Juergen Einsiedel, Philipp R. Weiglmeier, Paul Roesch, Peter Gmeiner, Stephan Schwarzinger, J. Biomol. Struct. Dyn. 2010, 28, 13-22. pdf

169    Synthesis of a ⁶⁸Ga-Labeled Peptoid-Peptide Hybrid for Imaging of Neurotensin Receptor Expression in Vivo. Simone Maschauer, Juergen Einsiedel, Carsten Hocke, Harald Huebner, Torsten Kuwert, Peter Gmeiner, and Olaf Prante, ACS Med. Chem. Lett. 2010, 1, 224-228. [doi>10.1021/ml1000728]

168    A Series of ¹⁸F-Labelled Pyridinylphenyl Amides as Subtype-Selective Radioligands for the Dopamine D3 Receptor. Carsten Hocke, Simone Maschauer, Harald Huebner, Stefan Loeber, Wolfgang Utz, Torsten Kuwert, Peter Gmeiner, and Olaf Prante, ChemMedChem 2010, 5, 941-948. [doi>10.1002/cmdc.201000067]

167    Click-Chemistry-Derived Tetracycline-Amino Acid Conjugates Exhibiting Exceptional Potency and Exclusive Recognition of the Reverse Tet Repressor. Igor Usai, Marcus Krueger, Juergen Einsiedel, Wolfgang Hillen, and Peter Gmeiner, ChemBioChem 2010, 11, 703-712. [doi>10.1002/cbic.200900710]

166    Tetracycline sensing using novel doxycycline derivatives immobilized on different surface plasmon resonance biosensor surfaces. Ulrike Andree, Erika Mueller-Seitz, Igor Usai, Stefan Loeber, Peter Gmeiner, Cornelius Wimmer, Wolfgang Hillen, Michael Petz, Bioanalysis 2010, 2, 217-227. [doi>10.4155/bio.09.176]

165    Labeling and Glycosylation of Peptides Using Click Chemistry: A General Approach to 18F-Glycopeptides as Effective Imaging Probes for Positron Emission Tomography. Simone Maschauer, Juergen Einsiedel, Roland Haubner, Carsten Hocke, Matthias Ocker, Harald Huebner, Torsten Kuwert, Peter Gmeiner, Olaf Prante, Angew. Chem. 2010, 122, 988-992, Angew. Chem. Int. Ed. 2010, 49, 976-979. [doi>10.1002/anie.200904137]

164    Engineering a GPCR-Ligand Pair That Simulates the Activation of D2L by Dopamine. Nuska Tschammer, Miriam Doerfler, Harald Huebner, and Peter Gmeiner, ACS Chemical Neuroscience 2010, 1, 25-35. [doi>10.1021/cn900001b]

163    Functional characterization of a partial loss-of-function mutation of the epithelial sodium channel (ENaC) associated with atypical cystic fibrosis. Regina Huber, Bettina Krueger, Alexei Diakov, Judit Korbmacher, Silke Haerteis, Juergen Einsiedel, Peter Gmeiner, Abul Kalam Azad, Harry Cuppens, Jean-Jacques Cassiman, Christoph Korbmacher, Robert Rauh, Cell. Physiol. Biochem. 2010, 25, 145-158.[doi>10.1159/000272059]

2009

162    Diarylpropane-1,3-dione Derivatives as TetR-Inducing Tetracycline Mimetics: Synthesis and Biological Investigations. Christian Kormann, Irina Pimenta, Stefan Loeber, Cornelius Wimmer, Harald Lanig, Timothy Clark, Wolfgang Hillen and Peter Gmeiner, ChemBioChem 2009, 10, 2924-2933. [doi>10.1002/cbic.200900564]

161    1,1′-Disubstituted Ferrocenes as Molecular Hinges in Mono- and Bivalent Dopamine Receptor Ligands. Daniela Huber, Harald Huebner, and Peter Gmeiner, J. Med. Chem. 2009, 52, 6860-6870. [doi>10.1021/jm901120h]

160    9-Aminoacridine derivatives and method using them for the treatment of autoimmune diseases. Carsten Korth, Ralf Klingenstein, Stefan Loeber, Peter Gmeiner, B. Kieseier, G. Meyer Zu Horste, Olaf Stuve. US 2009209516 (2009). pdf

159    Structural origins for selectivity and specificity in an engineered bacterial repressor-inducer pair. Michael A. Klieber, Oliver Scholz, Susanne Lochner, Peter Gmeiner, Wolfgang Hillen and Yves A. Muller, FEBS Journal 2009, 276, 5610-5621. [doi>10.1111/j.1742-4658.2009.07254.x]

158    Dopamine D2, D3, and D4 Selective Phenylpiperazines as Molecular Probes To Explore the Origins of Subtype Specific Receptor Binding. Katharina Ehrlich, Angela Gotz, Stefan Bollinger, Nuska Tschammer, Laura Bettinetti, Steffen Harterich, Harald Hubner, Harald Lanig, and Peter Gmeiner, J. Med. Chem. 2009, 52, 4923-4935. [doi>10.1021/jm900690y]

157    Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker. Pilar Rodriguez Loaiza, Stefan Loeber, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. 2009, 17, 5482-5487. [doi>10.1016/j.bmc.2009.06.041]

156    Novel triazolopeptides: chirospecific synthesis and conformational studies of proline derived analogs. Andreas Paul, Juergen Einsiedel, Reiner Waibel, Frank W. Heinemann, Karsten Meyer and Peter Gmeiner, Tetrahedron 2009, 65, 6156-6168. [doi>10.1016/j.tet.2009.05.045]

155    Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. Sabine Linz, Joerg Mueller, Harald Huebner, Peter Gmeiner and Reinhard Troschuetz, Bioorg. Med. Chem. 2009, 17, 4448-4458. [doi>10.1016/j.bmc.2009.05.015]

154    Heteroaryl-substituted 2-pyridylmethylamine derivatives. Harald Huebner, Peter Gmeiner, Stefan Bollinger. WO2009060030 (2009). pdf

153    The Azulene Framework as a Novel Arene Bioisostere: Design of Potent Dopamine D4 Receptor Ligands Inducing Penile Erection. Stefan Loeber, Nuska Tschammer, Harald Huebner, Maria Rosaria Melis, Antonio Argiolas and Peter Gmeiner, ChemMedChem 2009, 4, 325-328. [doi>10.1002/cmdc.200800395]

152    Quinpramine is a novel compound effective in ameliorating brain autoimmune disease. Mahendra P. Singh, Gerd Meyer zu Hoerste, Wei Hu, Anne K. Mausberg, Petra D. Cravens, Todd Eagar, Stefan Loeber, Ralf Klingenstein, Peter Gmeiner, Carsten Korth, Bernd C. Kieseier, Olaf Stueve, Experimental Neurology 2009, 215, 397-400. [doi>10.1016/j.expneurol.2008.10.001]

2008

151   Structural Characterisation of the E. coli Heat Stable Enterotoxin STh. Irena Matecko, Bjoern M. Burmann, Kristian Schweimer, Hubert Kalbacher, Juergen Einsiedel, Peter Gmeiner and Paul Roesch, The Open Spectroscopy Journal 2008, 2, 34-39. [doi>10.2174/1874383800802010034]

150    Preparation of indolizines and aza-analog derivatives thereof as CNS active compounds. Gmeiner, Peter; Huebner, Harald; Skultety, Marika. WO2008113559. pdf

149    Novel D3 Selective Dopaminergics Incorporating Enyne Units as Nonaromatic Catechol Bioisosteres: Synthesis, Bioactivity, and Mutagenesis Studies. Miriam Doerfler, Nuska Tschammer, Katharina Hamperl, Harald Huebner and Peter Gmeiner, J. Med. Chem. 2008, 51, 6829-6838. [doi>10.1021/jm800895v]

148    Novel Insights into GPCR-Peptide Interactions: Mutations in Extracellular Loop 1, Ligand Backbone Methylations and Molecular Modeling of Neurotensin Receptor 1. Steffen Haerterich, Susanne Koschatzky, Juergen Einsiedel and Peter Gmeiner, Bioorg. Med. Chem. 2008, 16, 9359-9368. [doi>10.1016/j.bmc.2008.08.051]

147    Proline Derived Spirobarbiturates as Highly Effective Beta-Turn Mimetics Incorporating Polar and Functionalizable Constraint Elements. Luelak Lomlim, Juergen Einsiedel, Frank W. Heinemann, Karsten Meyer and Peter Gmeiner, J. Org. Chem. 2008, 73, 3608-3611. [doi>10.1021/jo702573z]

146    Synthesis, Radiofluorination and In Vitro Evaluation of Pyrazolo[1,5-a]pyridine Based Dopamine D4 Receptor Ligands: Discovery of an Inverse Agonist Radioligand for PET. Olaf Prante, Rainer Tietze, Carsten Hocke, Stefan Loeber, Harald Huebner, Torsten Kuwert and Peter Gmeiner, J. Med. Chem. 2008, 51, 1800-1810. [doi>10.1021/jm701375u]

145    ¹⁸F-Labeled FAUC 346 and BP 897 Derivatives as Subtype-Selective Potential PET Radioligands for the Dopamine D3 Receptor. Carsten Hocke, Olaf Prante, Ismael Salama, Harald Huebner, Stefan Loeber, Torsten Kuwert and Peter Gmeiner, ChemMedChem 2008, 3, 788-793. [doi>10.1002/cmdc.200700327]

144    Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. Juergen Einsiedel, Harald Huebner, Maud Hervet, Steffen Haerterich, Susanne Koschatzky, and Peter Gmeiner, Bioorg. Med. Chem. Lett. 2008, 18, 2013-2018. [doi>10.1016/j.bmcl.2008.01.110]

143    Characterization of the Molecular Fragment that is Responsible for Agonism of Pergolide at Serotonin 5-HT2B and 5-HT2A Receptors. Tilo Goernemann, Harald Huebner, Peter Gmeiner, Reinhard Horowski, Klaus Peter Latté, Miroslav Flieger and Heinz H. Pertz, JPET 2008, 324, 1136-1145. [doi>10.1124/jpet.107.133165]

142    A simple chemical method for synthesizing malonyl hemiesters of 21-hydroxypregnanes, potential intermediates in cardenolide biosynthesis. Rodrigo M. Padua, Reiner Waibel, Serge Philibert Kuate, Pia K. Schebitz, Stefanie Hahn, Peter Gmeiner and Wolfgang Kreis, Steroids 2008, 73, 458-465. [doi>10.1016/j.steroids.2007.12.012]

141    Discovery of a dopamine D4 selective PET ligand taking advantage of a click chemistry based REM linker. Rainer Tietze, Stefan Loeber, Harald Huebner, Peter Gmeiner, Torsten Kuwert and Olaf Prante, Bioorg. Med. Chem. Lett. 2008, 18, 983-988. [doi>10.1016/j.bmcl.2007.12.026]

2007

140    Optimization of Click Chemistry Using Azide and Alkyne Scavenger Resins. Laurin Leeb, Peter Gmeiner and Stefan Loeber, QSAR Comb. Sci. 2007, 26, 1145-1150. [doi>10.1002/qsar.200740065]

139    Molecular Building Kit of Fused-Proline-Derived Peptide Mimetics Allowing Specific Adjustment of the Dihedral Psi Angle. Juergen Einsiedel, Harald Lanig, Reiner Waibel and Peter Gmeiner, J. Org. Chem. 2007, 72,  9102-9113. [doi>10.1021/jo701703e]

138    Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. Pilar Rodriguez Loaiza, Stefan Loeber, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. 2007, 15, 7248-7257. [doi>10.1016/j.bmc.2007.08.038]

137    In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D2-like dopamine receptors. Daniela Stark, Markus Piel, Harald Huebner, Peter Gmeiner, Gerhard Gruender and Frank Roesch, Bioorg. Med. Chem. 2007, 15, 6819-6829. [doi>10.1016/j.bmc.2007.07.017]

136    3,4,6-Tri-O-acetyl-2-deoxy-2-[¹⁸F]fluoroglucopyranosyl Phenylthiosulfonate: a Thiol-Reactive Agent for the Chemoselective ¹⁸F-Glycosylation of Peptides. Olaf Prante, Juergen Einsiedel, Roland Haubner, Peter Gmeiner, Hans-Juergen Wester, Torsten Kuwert and Simone Maschauer, Bioconjugate Chem. 2007, 18, 254-262. [doi>10.1021/bc060340v]

135    Dopamine D3 Receptor Ligands – Recent Advances in the Control of Subtype Selectivity and Intrinsic Activity. Frank M. Boeckler and Peter Gmeiner, Biochimica et Biophysica Acta, Biomembranes  2007, 1768, 871-887. [doi>10.1016/j.bbamem.2006.12.001]

134    Structure-Selectivity Investigations of D2-like Receptor Ligands by CoMFA and CoMSIA Guiding the Discovery of D3 Selective PET Radioligands. Ismail Salama, Carsten Hocke, Wolfgang Utz, Olaf Prante, Frank Boeckler, Harald Huebner, Torsten Kuwert and Peter Gmeiner, J. Med. Chem. 2007, 50, 489-500. [doi>10.1021/jm0611152]

2006

133    Preparation of piperazinylbutanamines and related compounds as selective dopamine D3 receptor inhibitors. Peter Gmeiner, Karin Schlotter and Harald Huebner. WO2006072430 A1. pdf  DE102004063797 A1. pdf

132    Preparation of ¹H-imidazo[4,5-b]pyridine-2-carboxamides and related compounds as D1 dopamine receptor inhibitors. Peter Gmeiner, Karin Schlotter, Harald Huebner, Dirk Schmidt and Monika Buchholz. WO2006050976 A1. pdf

131    PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain. Maria Rosaria Melis, Salvatora Succu, Fabrizio Sanna, Tiziana Melis, Maria Stefania Mascia, Cecile Enguehard-Gueiffier, Harald Huebner, Peter Gmeiner, Alain Gueiffier, Antonio Argiolas, Eur. J. Neurosci. 2006, 24, 2021-2030. [doi>10.1111/j.1460-9568.2006.05043.x]

130    Preparation of 9-aminoacridines and related compounds for the treatment of protein misfolding disorders. Carsten Korth, Ralf Klingenstein, Stefan Loeber and Peter Gmeiner, DE102005009909 A1. pdf

129    A Chimeric Ligand Approach Leading to Potent Antiprion Active Acridine Derivatives: Design, Synthesis and Biological Investigations. Silke Dollinger, Stefan Loeber, Ralf Klingenstein, Carsten Korth and Peter Gmeiner, J. Med. Chem. 2006, 49, 6591-6595. [doi>10.1021/jm060773j]

128    Triazolopeptides: chirospecific synthesis and cis/trans prolyl ratios of structural isomers. Andreas Paul, Holger Bittermann and Peter Gmeiner, Tetrahedron 2006, 62, 8919-8927. [doi>10.1016/j.tet.2006.07.007]

127    CoMFA and CoMSIA Investigations of Dopamine D3 Receptor Ligands Leading to the Prediction, Synthesis and Evaluation of Rigidized FAUC 365 Analogues. Ismail Salama, Karin Schlotter, Wolfgang Utz, Harald Huebner, Peter Gmeiner and Frank Boeckler, Bioorg. Med. Chem. 2006, 14, 5898-5912. [doi>10.1016/j.bmc.2006.05.025]

126    SCRF-DFT and NMR Comparison of Tetracycline and 5a,6-Anhydrotetracycline in Solution. Olaf G. Othersen, Reiner Waibel, Harald Lanig, Peter Gmeiner and Timothy Clark, J. Phys. Chem. B  2006, 110, 24766-24774. [doi>10.1021/jp064457s]

125    Dopamine D2 and D3 Receptors in Human Putamen, Caudate Nucleus, and Globus Pallidus. Philip Seeman, Alan Wilson, Peter Gmeiner and Shitij Kapur, Synapse 2006, 60, 205-211. [doi>10.1002/syn.20298]

124    Subtype Selective Tetracycline Agonists and their Application for a Two-Stage Regulatory System. Christian Berens, Susanne Lochner, Stefan Loeber, Igor Usai, Andreas Schmidt, Lars Drueppel, Wolfgang Hillen and Peter Gmeiner, ChemBioChem 2006, 7, 1320-1324. [doi>10.1002/cbic.200600226]

123    A Highly Practical RCM Approach towards a Molecular Building Kit of Spirocyclic Reverse Turn Mimics. Holger Bittermann, Frank Boeckler, Juergen Einsiedel and Peter Gmeiner, Chem. Eur. J. 2006, 12, 6315-6322. [doi>10.1002/chem.200600432]

122    A gene regulation system with four distinct expression levels. Christel Krueger, Christina Danke, Klaus Pfleiderer, Wolfgang Schuh, Hans-Martin Jaeck, Susanne Lochner, Peter Gmeiner, Wolfgang Hillen and Christian Berens, J. Gene Med. 2006, 8, 1037-1047. [doi>10.1002/jgm.932]

121    A Consecutive Diels-Alder Approach toward a Tet Repressor Directed Combinatorial Library. Christian Kormann, Frank W. Heinemann and Peter Gmeiner, Tetrahedron 2006, 62, 6899-6908. [doi>10.1016/j.tet.2006.04.092]

120    Fancy Bioisosteres: Novel Paracyclophane Derivatives as Super-Affinity Dopamine D3 Receptor Antagonists. Karin Schlotter, Frank Boeckler, Harald Huebner and Peter Gmeiner, J. Med. Chem. 2006, 49, 3628-3635. [doi>10.1021/jm060138d]

119    2-[(4-Phenylpiperazin-1-yl)methyl]imidazo(di)azines as Selective D4-Ligands. Induction of Penile Erection by 2-[4-(2-Methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a Potent and Selective D4 Partial Agonist. Cecile Enguehard-Gueiffier, Harald Huebner, Ahmed El Hakmaoui, Hassan Allouchi, Peter Gmeiner, Antonio Argiolas, Maria Rosaria Melis and Alain Gueiffier, J. Med. Chem. 2006, 49, 3938-3947. [doi>10.1021/jm060166w]

118    Tricyclic antidepressants, quinacrine and a novel, synthetic chimera thereof clear prions by destabilizing detergent-resistant membrane compartments. Ralf Klingenstein, Stefan Loeber, Pekka Kujala, Susan Godsave, S. Rutger Leliveld, Peter Gmeiner, Peter J. Peters and Carsten Korth, J. Neurochem. 2006, 98, 748-759. [doi>10.1111/j.1471-4159.2006.03889.x]

117    Synthesis and Biological Investigations of Dopaminergic Partial Agonists Preferentially Recognizing the D4 Receptor Subtype. Stefan Loeber, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. Lett. 2006, 16, 2955-2959. [doi>10.1016/j.bmcl.2006.02.075]

116    Preparation of piperazinylalkyl triazolecarboxamides as adrenergic and dopaminergic agents. Peter Gmeiner, Harald Huebner and Maria del Pilar Rodriguez Loaiza, DE102004039065 A1. 

115    Preparation of 2-indolizinecarboxamides and related compounds as central nervous system agents. Peter Gmeiner, Harald Huebner, Laura Bettinetti and Karin Schlotter, WO2006015737 A1.

114    Click Chemistry on Solid Phase: Parallel Synthesis of N-Benzyltriazole Carboxamides as Super-Potent G-Protein Coupled Receptor Ligands. Pilar Rodriguez Loaiza, Stefan Loeber, Harald Huebner and Peter Gmeiner, J. Comb. Chem. 2006, 8, 252-261. [doi>10.1021/cc050127q]

113    Syntheses and radiofluorination of two derivatives of 5-cyano-indole as selective ligands for the dopamine subtype-4 receptor. Rainer Tietze, Carsten Hocke, Stefan Loeber, Harald Huebner, Torsten Kuwert, Peter Gmeiner and Olaf Prante,  J. Labelled Cmpds. Radiopharm. 2006, 49, 55-70. pdf

112    Bicyclic Melatonin Receptor Agonists Containing a Ring-junction Nitrogen: Synthesis, Biological Evaluation, and Molecular Modeling of the Putative Bioactive Conformation. Jan Elsner, Frank Boeckler, Kathryn Davidson, David Sugden and Peter Gmeiner, Bioorg. Med. Chem. 2006, 14, 1949-1958. [doi>10.1016/j.bmc.2005.10.042]

111    Chirospecific Synthesis of Spirocyclic Beta-Lactams and their Characterization as Potent Type II Beta-Turn Inducing Peptide Mimetics. Holger Bittermann and Peter Gmeiner, J. Org. Chem., 2006, 71, 97-102. [doi>10.1021/jo0517287]

110    Tissue distribution of radioiodinated FAUC 113: Assessment of a pyrazolo[1,5-a]pyridine based dopamine D4 receptor radioligand candidate. Olaf Prante, Carsten Hocke, Stefan Loeber, Harald Huebner, Peter Gmeiner and Torsten Kuwert,  Nuclear Medicine 2006, 45, 41-48. pdf

109    The Structural Evolution of Dopamine D3 Receptor Ligands – Structure-Activity Relationships and Selected Neuropharmacological Aspects. Frank Boeckler and Peter Gmeiner, Pharmacology & Therapeutics, 2006, 112, 281-333. [doi>10.1016/j.pharmthera.2006.04.007]

2005

108    Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents. Carsten Hocke, Olaf Prante, Stefan Loeber, Harald Huebner, Peter Gmeiner and Torsten Kuwert, Bioorg. Med. Chem. Lett. 2005, 15, 4819-4823. [doi>10.1016/j.bmcl.2005.07.037]

107    Pharmacophore-Guided Drug Discovery Investigations Leading to Bioactive 5-Aminotetrahydropyrazolopyridines. Implications for the Binding Mode of Heterocyclic Dopamine D3 Receptor Agonists. Jan Elsner, Frank Boeckler, Frank W. Heinemann, Harald Huebner and Peter Gmeiner, J. Med. Chem. 2005, 48, 5771-5779. [doi>10.1021/jm0503805]

106    Fancy Bioisosteres: Metallocene-Derived G-Protein-Coupled Receptor Ligands with Subnanomolar Binding Affinity and Novel Selectivity Profiles. Karin Schlotter, Frank Boeckler, Harald Huebner and Peter Gmeiner. J. Med. Chem.  2005, 48, 3696-3699. [doi>10.1021/jm050170s]

105    Chirospecific and Subtype Selective Dopamine Receptor Binding of Heterocyclic Methoxynaphthamide Analogs. Laura Bettinetti, Harald Huebner and Peter Gmeiner, Arch. Pharm. Chem. Life Sci. 2005, 338, 276-280. [doi>10.1002/ardp.200400997]

104    Fancy Bioisosteres: Synthesis, SAR and Pharmacological Investigations of Novel Nonaromatic Dopamine D3 Receptor Ligands. Carola Lenz, Frank Boeckler, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. 2005, 13, 4434-4442. [doi>10.1016/j.bmc.2005.04.047]

103    CoMFA and CoMSIA Investigations Revealing Novel Insights into the Binding Modes of Dopamine D3 Receptor Agonists. Frank Boeckler, Ursula Ohnmacht, Thomas Lehmann, Wolfgang Utz, Harald Huebner and Peter Gmeiner, J. Med. Chem. 2005, 48, 2493-2508. [doi>10.1021/jm049269+]

102    Parallel Synthesis and Biological Screening of Dopamine Receptor Ligands Taking Advantage of a Click Chemistry Based BAL Linker. Laura Bettinetti, Stefan Loeber, Harald Huebner and Peter Gmeiner, J. Comb. Chem. 2005, 7, 309-316. [doi>10.1021/cc049860s]

101    Modeling the Similarity and Divergence of Dopamine D2-like Receptors and Identification of Validated Ligand-Receptor Complexes. Frank Boeckler, Harald Lanig and Peter Gmeiner, J. Med. Chem. 2005, 48, 694-709. [doi>10.1021/jm049612a]

100    Fancy bioisosteres: synthesis and dopaminergic properties of the endiyne FAUC 88 as a novel non-aromatic D3 agonist. Carola Lenz, Christian Haubmann, Harald Huebner, Frank Boeckler and Peter Gmeiner, Bioorg. Med. Chem. 2005, 13, 185-191. [doi>10.1016/j.bmc.2004.09.044]

2004

99    Evaluation of Lactam Bridged Neurotensin Analogues Adjusting ψ(Pro10) Close to the Experimentally Derived Bioactive Conformation of NT(8-13). Holger Bittermann, Juergen Einsiedel, Harald Huebner and Peter Gmeiner, J. Med. Chem. 2004, 47, 5587-5590. [doi>10.1021/jm049644y]

98    Certain 1,4-Disubstituted Aromatic Piperidines and Piperazines with Extreme Selectivity for the Dopamine D4 Receptor Interact with a Common Receptor Microdomain. Sandhya Kortagere, Peter Gmeiner, Harel Weinstein and John A. Schetz, Mol. Pharmacol. 2004, 66, 1491-1499. [doi>10.1124/mol.104.001321]

97    Structure based design of Tet repressor to optimize a new inducer specificity. Eva-Maria Henssler, Oliver Scholz, Susanne Lochner, Peter Gmeiner and Wolfgang Hillen, Biochemistry 2004, 43, 9512-9518. [doi>10.1021/bi049682j]

96    Synthesis and Radioiodination of Selective Ligands for the Dopamine D3 Receptor Subtype. Carsten Hocke, Olaf Prante, Stefan Loeber, Harald Huebner, Peter Gmeiner and Torsten Kuwert, Bioorg. Med. Chem. Lett. 2004, 14, 3963-3966. [doi>10.1016/j.bmcl.2004.05.052]

95    Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing. Thomas Hussenether, Harald Huebner, Peter Gmeiner and Reinhard Troschuetz, Bioorg. Med. Chem. 2004, 12, 2625-2637. [doi>10.1016/j.bmc.2004.03.023]

94    Click Chemistry on Solid Support: Synthesis of a New REM Resin and Application for the Preparation of Tertiary Amines. Stefan Loeber and Peter Gmeiner, Tetrahedron 2004, 60, 8699-8702. [doi>10.1016/j.tet.2004.05.099]

93    FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Frank Boeckler, H. Russig, W. Zhang, Stefan Loeber, Harald Huebner, B. Ferger, Peter Gmeiner and J. Feldon, Psychopharmacology 2004, 175, 7-17. [doi>10.1007/s00213-004-1782-1]

92    Preparation of arylpiperazinylbutylheteroarene carboxamides and related compounds as dopamine D3 ligands for the treatment of central nervous system diseases. Peter Gmeiner, Harald Huebner and Karin Schlotter, WO2004004729 A1. pdf

91    Practical ex-chiral-pool methodology for the synthesis of dopaminergic tetrahydroindoles. Markus Bergauer, Harald Huebner and Peter Gmeiner, Tetrahedron 2004, 60, 1197-1204. [doi>10.1016/j.tet.2003.11.041]

90    Analogues of FAUC 73 revealing new insights into the structural requirements of nonaromatic dopamine D3 receptor agonists. Carola Lenz, Frank Boeckler, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. 2004, 12, 113-117. [doi>10.1016/j.bmc.2003.10.011]

2003

89    Enantiospecific synthesis and receptor binding of novel dopamine receptor ligands employing natural 4-hydroxyproline as a practical and flexible building block. Cornelia Heindl, Harald Huebner and Peter Gmeiner, Tetrahedron: Asymmetry 2003, 14, 3153-3172. [doi>10.1016/j.tetasy.2003.08.020]

88    Ex-chiral pool synthesis and receptor binding studies of 4-substituted prolinol derivatives. Cornelia Heindl, Harald Huebner and Peter Gmeiner, Tetrahedron: Asymmetry 2003, 14, 3141-3152. [doi>10.1016/j.tetasy.2003.08.019]

87    Attenuation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) neurotoxicity by the novel selective dopamine D3-receptor partial agonist FAUC 329 predominantly in the nucleus accumbens of mice. Frank Boeckler, Andreas Leng, Anna Mura, Laura Bettinetti, Joram Feldon, Peter Gmeiner and Boris Ferger, Biochem. Pharmacol. 2003, 66, 1025-1032. [doi>10.1016/S0006-2952%2803%2900451-9]

86    Stereocontrolled Dopamine Receptor Binding and Subtype Selectivity of Clebopride Analogues Synthesized from Aspartic Acid. Juergen Einsiedel, Klaus Weber, Christoph Thomas, Thomas Lehmann, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. Lett. 2003, 13, 3293-3296. [doi>10.1016/S0960-894X%2803%2900678-4]

85    Click Linker: Efficient and High-Yielding Synthesis of a New Family of SPOS Resins by 1,3-Dipolar Cycloaddition. Stefan Loeber, Pilar Rodriguez-Loaiza and Peter Gmeiner*, Org. Lett. 2003, 5, 1753. [doi>10.1021/ol034520l]

84    Synthesis and Dopamine Receptor Binding of Some Pyrazolo[3′,4′:6,7]azepino[5,4,3-cd]indoles. Peter Gmeiner, Harald Huebner, Kayed A. Abu Safieh, Ismail I. Fasfous, Mustafa M. El-Abadelah*, Salim S. Sabri and Wolfgang Voelter, Heterocycles 2003, 60, 1339.pdf

83    Synthesis of dihydrooxazole analogues derived from linezolid. Juergen Einsiedel, Christoph Schoerner and Peter Gmeiner*, Tetrahedron 2003, 59, 3403. [doi>10.1016/S0040-4020%2803%2900490-3]

82    Cyclic Amidines as Benzamide Bioisosteres: EPC Synthesis and SAR Studies Leading to the Selective Dopamine D4 Receptor Agonist FAUC 312. Juergen Einsiedel, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2003, 13, 851. [doi>10.1016/S0960-894X%2803%2900004-0]

81    A General Approach to Dehydro-Freidinger Lactams: Ex-Chiral Pool Synthesis and Spectroscopic Evaluation as Potential Reverse Turn Inducers. Tobias Hoffmann, Reiner Waibel and Peter Gmeiner*, J. Org. Chem. 2003, 68, 62. [doi>10.1021/jo0261653]

2002

80    Analogs of the dopamine D4 receptor ligand FAUC 113 with planar- and central-chirality. Stefan Loeber, Birgit Ortner, Laura Bettinetti, Harald Huebner and Peter Gmeiner*, Tetrahedron: Asymmetry 2002, 13, 2303. [doi>10.1016/S0957-4166%2802%2900639-0]

79    Interactive SAR Studies: Rational Discovery of Super-Potent and Highly Selective Dopamine D3 Receptor Antagonists and Partial Agonists. Laura Bettinetti, Karin Schlotter, Harald Huebner and Peter Gmeiner*, J. Med. Chem. 2002, 45, 4594. [doi>10.1021/jm025558r]

78    Fused Azaindole Derivatives: Molecular Design, Synthesis and in vitro Pharmacology Leading to the Preferential Dopamine D3 Receptor Agonist FAUC 725. Stefan Loeber , Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2002, 12, 2377. [doi>10.1016/S0960-894X%2802%2900390-6]

77    Short and Efficient Synthesis of Homo-Freidinger Lactams: An Olefin Metathesis Approach Towards Conformationally Restricted Beta-Amino Acid Analogues. Tobias Hoffmann and Peter Gmeiner*, Synlett 2002, 1014.pdf

76    2,4-Disubstituted Pyrroles: Synthesis, Traceless Linking and Pharmacological Investigations Leading to the Dopamine D4 Receptor Partial Agonist FAUC 356. Markus Bergauer, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2002, 12, 1937. [doi>10.1016/S0960-894X%2802%2900316-5]

75    Phenylpiperazinylmethylindolecarboxylates and Derivatives as Selective D4-Ligands. Annette Moll, Harald Huebner, Peter Gmeiner and Reinhard Troschuetz*, Bioorg. Med. Chem. 2002, 10, 1671. [doi>10.1016/S0968-0896%2802%2900042-1]

74    Traceless Linking of Pyrroles: General Methology and Solid Phase Supported Functionalizations. Markus Bergauer and Peter Gmeiner*, Synthesis 2002, 274. [doi>10.1055/s-2002-19813]

73    Di- and Trisubstituted Pyrazolo[1,5-a]pyridine Derivatives: Synthesis, Dopamine Receptor Binding and Ligand Efficacy. Stefan Loeber, Tarek Aboul-Fadl, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2002, 12, 633. [doi>10.1016/S0960-894X%2801%2900814-9]

2001

72    Planar Chiral Indoles: Synthesis and Biological Effects of the Enantiomers. Birgit Ortner, Harald Huebner and Peter Gmeiner*, Tetrahedron: Asymmetry 2001, 12, 3205. [doi>10.1016/S0957-4166%2801%2900558-4]

71    Diethoxymethyl Protected Pyrroles: Synthesis and Regioselective Transformations. Markus Bergauer and Peter Gmeiner*, Synthesis 2001, 2281. [doi>10.1055/s-2001-18445]

70    Dopaminergic 7-Aminotetrahydroindolizines: Ex-Chiral Pool Synthesis and Preferential D3 Receptor Binding. Thomas Lehmann, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2001, 11, 2863. [doi>10.1016/S0960-894X%2801%2900564-9]

69    Synthesis and in vitro Evaluation of Iodine Labelled Pyrazolo[1,5-a]pyridines as Highly Selective Dopamine D4 Receptor Ligands. Olaf Prante, Stefan Loeber, Harald Huebner, Peter Gmeiner and Torsten Kuwert, J. Labelled Cpd. Radiopharm. 2001, 44, 849. [doi>10.1002/jlcr.508]

68    Rationally Based Efficacy Tuning of Selective Dopamine D4 Receptor Ligands Leading to the Complete Antagonist 2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). Stefan Loeber, Harald Huebner, Wolfgang Utz and Peter Gmeiner*, J. Med. Chem. 2001, 44, 2691. [doi>10.1021/jm015522j]

67    Rational Molecular Design and EPC Synthesis of a Type VI Beta-Turn Inducing Peptide Mimetic. Tobias Hoffmann, Harald Lanig, Reiner Waibel and Peter Gmeiner*, Angew. Chem. 2001, 113, 3465, Angew. Chem. Int. Ed. 2001, 40, 3361. [doi>10.1002/1521-3773(20010917)40:18<3361::AID-ANIE3361>3.0.CO;2-9]

66    Benzamide Bioisosteres Incorporating Dihydroheteroazole Substructures: EPC Synthesis and SAR Leading to a Selective Dopamine D4 Receptor Partial Agonist (FAUC 179). Juergen Einsiedel, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2001, 11, 2533. [doi>10.1016/S0960-894X%2801%2900484-X]

65    Preparation of Indole Derivatives by Solid Phase Synthesis. Michael Arlt, Peter Gmeiner and Johannes Kraxner, WO2001023353 A2. pdf

64    Indoloparacyclophanes: Synthesis and Dopamine Receptor Binding of a Novel Arylbioisostere. Birgit Ortner, Reiner Waibel and Peter Gmeiner*, Angew. Chem. 2001, 113, 1323, Angew. Chem. Int. Ed. 2001, 40, 1283. [doi>10.1002/1521-3757(20010401)113:7<1323::AID-ANGE1323>3.0.CO;2-I]

63    Comparative Molecular Field Analysis of Dopamine D4 Receptor Antagonists Including 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo[2,3-b]pyridine (L-745,870), and Clozapine. Harald Lanig, Wolfgang Utz and Peter Gmeiner*, J. Med. Chem. 2001, 44, 1151. [doi>10.1021/jm001055e]

2000

62    Effective and Variable Functionalization of Pyrazolo[1,5-a]pyridines Involving Palladium-Catalyzed Coupling Reactions. Tarek Aboul-Fadl, Stefan Loeber and Peter Gmeiner*, Synthesis 2000, 1727. [doi>10.1055/s-2000-8215]

61    Cyanoindole Derivatives as Highly Selective Dopamine D4 Receptor Partial Agonists: Solid-Phase Synthesis, Binding Assays, and Functional Experiments. Harald Huebner, Johannes Kraxner and Peter Gmeiner*, J. Med. Chem. 2000, 43, 4563. [doi>10.1021/jm0009989]

60    Azepino- and Diazepinoindoles: Synthesis and Dopamine Receptor Binding Profiles. Johannes Kraxner, Harald Huebner and Peter Gmeiner*, Arch. Pharm. Pharm. Med. Chem. 2000, 333, 287. [doi>10.1002/1521-4184(20009)333:9<287::AID-ARDP287>3.0.CO;2-R]

59    Enantiopure 4- and 5-Aminopiperidin-2-ones: Regiocontrolled Synthesis and Conformational Characterization as Bioactive Beta-Turn Mimetics. Klaus Weber, Ursula Ohnmacht and Peter Gmeiner*, J. Org. Chem. 2000, 65, 7406. [doi>10.1021/jo000555c]

58    Phenyloxazoles and Phenylthiazoles as Benzamide Bioisosteres: Synthesis and Dopamine Receptor Binding Profiles. Juergen Einsiedel, Christoph Thomas, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 2000, 10, 2041. [doi>10.1016/S0960-894X%2800%2900405-4]

57    Synthesis of Enantiopure 8-Aminomethylindolizines from Glutamine by Stereoelectronically Controlled Cationic Cyclization. Thomas Lehmann and Peter Gmeiner*, Heterocycles 2000, 53, 1371.pdf

56    Regiocontrolled Annellation Reactions Starting from Diethoxymethyl Protected Indole. Johannes Kraxner and Peter Gmeiner*, Synthesis 2000, 1081. [doi>10.1055/s-2000-6329]

55    Treatment of N,N-Dibenzylamino Alcohols with Sulfonyl Chloride Leads to Rearranged Beta-Chloro Amines, Precursors to Beta-Amino Acids, and Not to Tetrahydroisoquinolines. Klaus Weber, Stephan Kuklinkski and Peter Gmeiner*, Org. Lett. 2000, 2, 647. [doi>10.1021/ol991402i]

54    Conjugated Enynes as Nonaromatic Catechol Bioisosteres: Synthesis, Binding Experiments and Computational Studies of Novel Dopamine Receptor Agonists Recognizing Preferentially the D3 Subtype. Harald Huebner, Christian Haubmann, Wolfgang Utz and Peter Gmeiner*, J. Med. Chem. 2000, 43, 756. [doi>10.1021/jm991098z]

53    Traceless Linking of Indoles: General Methodology and Application to Solid Phase Supported Mannich and Stille Reactions. Johannes Kraxner, Michael Arlt and Peter Gmeiner*,  Synlett 2000, 125. [doi>10.1055/s-2000-6439]

1999

52    Piperidinylpyrroles: Design, Synthesis and Binding Properties of Novel and Selective Dopamine D4 Receptor Ligands. Christian Haubmann, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 1999, 9, 3143. [doi>10.1016/S0960-894X%2899%2900540-5]

51    2,2-Dicyanovinyl as a Nonaromatic Aryl Bioisostere: Synthesis, Binding Experiments and SAR Studies of Highly Selective Dopamine D4 Receptor Ligands. Christian Haubmann, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett., 1999, 9, 1969. [doi>10.1016/S0960-894X%2899%2900302-9]

50    Chemo- and Regioselective Syntheses of Enantiopure Aminopyrrolidinones as Building Blocks for Constrained Peptidomimetics. Thomas Lehmann, Dorothee Michel, Markus Glaenzel, Reiner Waibel and Peter Gmeiner*, Heterocycles 1999, 51, 1389.pdf

49    Enantio- and Diastereocontrolled Dopamine D1, D2, D3 and D4 Receptor Binding of N-(3-Pyrrolidinylmethyl)benzamides Synthesized from Aspartic Acid. Christoph Thomas, Harald Huebner and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 1999, 9, 841. [doi>10.1016/S0960-894X%2899%2900086-4]

48    Azaindole Derivatives with High Affinity for the Dopamine D4 Receptor: Synthesis, Ligand Binding Studies and Comparison of Molecular Electrostatic Potential Maps. Stefan Loeber, Harald Huebner and Peter Gmeiner, Bioorg. Med. Chem. Lett. 1999, 9, 97. [doi>10.1016/S0960-894X%2898%2900692-1]

47    Ex-Chiral Pool Synthesis of Aminooxazepinones as Conformationally Restricted Beta-Amino Acid Analogs. Dorothee Michel, Reiner Waibel and Peter Gmeiner*, Heterocycles 1999, 51, 365.pdf

46    Ex-Chiral Pool Synthesis and Pharmacological Aspects of 3-Pyrrolidinyl-isoxazoles. Christoph Thomas, Ursula Ohnmacht, Katrin Zahn, Klaus Mohr and Peter Gmeiner*, Pharmazie 1999, 54, 248.pdf

45    [³H]Pramipexole: A Selective Radioligand for the High Affinity Dopamine D2 Receptor in Bovine Striatal Membranes. Ursula Ohnmacht, Christian Traenkle, Klaus Mohr and Peter Gmeiner*, Pharmazie 1999, 54, 294.pdf

1998

44    Beta-Analogs of PLG (L-Prolyl-L-Leucyl-Glycinamide): Ex-Chiral Pool Syntheses and Dopamine D2 Receptor Modulating Effects. Christoph Thomas, Ursula Ohnmacht, Martin Niger and Peter Gmeiner*, Bioorg. Med. Chem. Lett. 1998, 8, 2885.pdf

43    A Practical Ex-Chiral-Pool Synthesis of Beta-Proline and Homo-Beta-Proline. Christoph Thomas, Florian Orecher and Peter Gmeiner*, Synthesis 1998, 1491.pdf

42    Homo-Freidinger Lactams: Stereoselective Synthesis of 4-Aminopiperidin-2-one Derivatives from Aspartic Acid. Klaus Weber and Peter Gmeiner*, Synlett 1998, 885.pdf

1997

41 Selective Transformations of N,N-Dibenzyl Protected Asparagine and Aspartic Acid Derivatives. Peter Gmeiner, in Enantioselective Synthesis of Beta-Amino Acids (Ed. Eusebio Juaristi), Wiley-VCH, New York 1997.

1996

40    Diethoxymethyl Protected Indoles: Synthesis and Regioselective Trans¬formations. Peter Gmeiner*, Johannes Kraxner and Bernd Bollinger, Synthesis 1996, 1196.pdf

39    Synthesis and Stereochemistry of Oxazolo[4′,5′:1,2]benz[5,4,3-c,d]indole Derivatives as Intermediates on the Way to a Selective Dopamine Autoreceptor Agonist. Peter Gmeiner*, Bernd Bollinger and Hermann Lotter, J. Heterocyclic Chem. 1996, 33, 481.pdf

1995

38    Synthesis of Optically Active Alpha,Beta-Disubstituted Beta-Amino Nitriles and Beta-Amino Acids Starting from Asparagine. Peter Gmeiner*, Evi Hummel and Christian Haubmann, Liebigs Ann. Chem. 1995, 1987.pdf

37    Synthesis and Dopamine Receptor Binding Studies of Homochiral 8 Aminopyrido[1,2-a]indoles. Peter Gmeiner*, Annerose Kaertner and Joachim Mierau, Arch. Pharm. (Weinheim) 1995, 328, 626.pdf

36    Synthesis, Pharmacological Investigation and Computational Studies on a Tricyclic Ergoline Analog with Selective Dopamine Autoreceptor Activity. Peter Gmeiner*, Bernd Bollinger, Joachim Mierau and Georg Hoefner, Arch. Pharm. (Weinheim) 1995, 328, 609.pdf

35    Regioselective Transformation of Malic Acid: A Practical Method for the Con¬struction of Enantiomerically Pure Indolizidines. Peter Gmeiner* and Dagmar Junge, J. Org. Chem. 1995, 60, 3910.pdf

34    Synthesis and Dopamine Receptor Binding of 3-Phenylazepino[5,4,3-c,d]indole Derivatives. Peter Gmeiner*, Josef Sommer and Georg Hoefner, Arch. Pharm. (Weinheim) 1995, 328, 329.pdf

33    Synthesis of (S)-3,4-Diaminobutanenitriles as Precursors for 3-Amino-GABA Derivatives. Peter Gmeiner*, Evi Hummel, Christian Haubmann and Georg Hoefner, Arch. Pharm. (Weinheim) 1995, 328, 265.pdf

32    Diethoxymethyl: A Useful Nitrogen-Protecting Group for Lactams and Amides. Peter Gmeiner* and Bernd Bollinger, Synthesis 1995, 168.pdf

31    2-Dibenzylaminobutane-1,4-diol: A Versatile Intermediate for a Chirospecific Beta-Amino Acid Synthesis. Peter Gmeiner*, Florian Orecher, Christoph Thomas and Klaus Weber, Tetrahedron Lett. 1995, 36, 381.pdf

30    2-Dibenzylaminobutane-1,4-diol: An Effective Chiral Building Block for the Synthesis of 1,2-Amino Alcohols. Peter Gmeiner* and Annerose Kaertner, Synthesis 1995, 83.pdf

1994

29    Enantiomerically Pure Amino Alcohols and Diamino Alcohols from L-Aspartic Acid. Application to the Synthesis of Epi- and Diepislaframine. Peter Gmeiner*, Dagmar Junge and Annerose Kaertner, J. Org. Chem. 1994, 59, 6766.pdf

28    Novel HO-DPAT (Hydroxy-2-dipropylaminotetralin) Isomers: Stereoselective Synthesis and Receptor Binding Studies. Peter Gmeiner*, Evi Hummel and Joachim Mierau, Bioorg. Med. Chem. Lett. 1994, 4, 2589.pdf

27    Diastereoselective Synthesis of the C2-Symmetric 2,3-Diaminotetralin via Electro¬philic Amination. Peter Gmeiner* and Evi Hummel, Synthesis 1994, 1026.pdf

26    Asymmetric Synthesis of Beta-Aminotetralins by Electrophilic Amination. Peter Gmeiner* and Bernd Bollinger, Tetrahedron 1994, 50, 10909.pdf

25    Bi- und tricyclische Ergolinanaloge mit dopaminergen Eigenschaften. Peter Gmeiner, Pharmazie in unserer Zeit 1994, 23, 169.pdf

24    Selektive Dopamin D-2 Autorezeptor Agonisten mit 8-Azaindol Substruktur: Synthese und theoretische Untersuchungen. Peter Gmeiner* und Josef Sommer, Arch. Pharm. (Weinheim) 1994, 327, 435.pdf

1993

23    Practical EPC Synthesis of 1,2- and 1,3-Amino Alcohols. Peter Gmeiner*, Annerose Kaertner and Dagmar Junge, Tetrahedron Lett. 1993, 34, 4325.pdf

22    Dopamine Autoreceptor Agonists: Computational Studies, Synthesis and Biological Investigations. Peter Gmeiner*, Josef Sommer, Joachim Mierau and Georg Hoefner, Bioorg. Med. Chem. Lett. 1993, 3, 1477.pdf

1992

21    Tricyclic Azaergoline Analogues: Synthesis, Structural Modifications, and Pharmacological Studies. Peter Gmeiner*, Josef Sommer, Georg Hoefner and Joachim Mierau, Arch. Pharm. (Weinheim) 1992, 325, 649.pdf

20    Synthesis of Amines and Amino Alcohols by Electrophilic Amination and Highly Stereoselective Reduction. Peter Gmeiner* and Bernd Bollinger, Liebigs Ann. Chem. 1992, 273.pdf

19    Enantiomerically Pure Aminoindolizines: Bicyclic Ergoline Analogues with Dopamine Autoreceptor Activity. Peter Gmeiner*, Joachim Mierau and Georg Hoefner, Arch. Pharm. (Weinheim) 1992, 325, 57.pdf

1991

18    Efficient Methodology for the Preparation of Beta-Aminotetralin Derivatives via Electrophilic Amination. Peter Gmeiner* and Bernd Bollinger, Tetrahedron Lett. 1991, 32, 5927.pdf

17    Stereoelectronically Controlled Cyclization Reactions on the Way to peri-Fused Tetrahydropyrazolo[1,5-a]pyridines as Aza Analogs of Ergoline Partial Structures. Peter Gmeiner* and Josef Sommer, Liebigs Ann. Chem. 1991, 921.pdf

16    Synthesis of Chiral Indolizines as Bicyclic Ergoline Analogues. Peter Gmeiner, Heterocycles 1991, 32, 1499.pdf

15    An Efficient and Practical EPC Synthesis of Beta-Amino Acids from L-Asparagine. Peter Gmeiner, Arch. Pharm. (Weinheim) 1991, 324, 551.pdf

14    Efficient EPC Synthesis of Beta-Aminobutanoic Acid. Peter Gmeiner, Liebigs Ann. Chem. 1991, 501.pdf

1990

13    Synthesis of Tricyclic Azaergoline Analogues. Peter Gmeiner* and Josef Sommer, Arch. Pharm. (Weinheim) 1990, 323, 991.pdf

12    General Synthesis of Enantiomerically Pure Beta-Amino Acids. Peter Gmeiner, Tetrahydron Lett. 1990, 31, 5717.pdf

11    New and Efficient Synthesis of 5,6,7,8-Tetrahydroindolizidines. Application to the Synthesis of Pharmacologically Relevant Chiral Aminoderivatives from L Asparagine. Peter Gmeiner* and Holger Lerche, Heterocycles 1990, 31, 9.pdf

10    An Efficient and Practical Total Synthesis of (+)-Vincamine from L-Aspartic Acid. Peter Gmeiner, Paul L. Feldman, Margaret Y. Chu-Moyer and Henry Rapoport*, J. Org. Chem. 1990, 55, 3068.pdf

1988

9    Azaindol-Derivate II: Synthese und analgetische Wirkung von Pyrazolo[1,5-a]pyridinen. Peter Gmeiner* und Juergen Schuenemann, Arch. Pharm. (Weinheim) 1988, 321, 517.pdf

8    Azaindol-Derivate I: Asymmetrische Synthese einer neuen Alpha-Aminosaeure. Peter Gmeiner* und Josef Sommer, Arch. Pharm. (Weinheim) 1988, 321, 505.pdf

7    Synthese von ZNS-Wirkstoffen: Pyran-, thiopyran- und piperidinanellierte Oxa-carbabenzomorphane. Fritz Eiden* und Peter Gmeiner, Arch. Pharm. (Weinheim) 1988, 321, 397.pdf

6    Oxabenzomorphane: Ãœber ZNS-Wirkungen von Hexahydro-2,7-methano-1,5-benzoxazoninen. Fritz Eiden*, Peter Gmeiner und Juergen Schuenemann, sowie  Rosemarie Ruhoff und Meinhart Zenk, Arch. Pharm. (Weinheim) 1988, 321, 325.pdf

5    Oxabenzomorphane: Synthese ZNS-wirksamer Hexahydro-2,7-methano-1,5-benzoxazonine. Fritz Eiden* und Peter Gmeiner, Arch. Pharm. (Weinheim) 1988, 321, 321.pdf

4    Preparation of 2,3,4,5,6,7-hexahydro-2,7-methano-1,5-(and 1,4)-benzoxazonines as analgesics and muscle relaxants. Friedrich Eiden, Peter Gmeiner und Juergen Schuenemann, DE3630539 A1. pdf

3    Regio- und diastereoselektive Synthesen von Hexahydro-4a,9-propanoxanthenonen. Fritz Eiden*, Peter Gmeiner und Hermann Lotter, Liebigs Ann. Chem. 1988, 125.pdf

1987

2    Oxabenzomorphane: Synthese, Reaktionen und ZNS-Wirkung von 2,6-Methano-1-benzoxocinen. Fritz Eiden* und Peter Gmeiner, Arch. Pharm. (Weinheim) 1987, 320, 213.pdf

1986

1    Synthese anellierter Oxabenzomorphane. Fritz Eiden* und Peter Gmeiner, Arch. Pharm. (Weinheim) 1986, 319, 431. pdf