| Year |
Citation |
Score |
| 2024 |
Drakopoulos A, Koszegi Z, Seier K, Hübner H, Maurel D, Sounier R, Granier S, Gmeiner P, Calebiro D, Decker M. Design, Synthesis, and Characterization of New δ Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors. Journal of Medicinal Chemistry. 67: 12618-12631. PMID 39044606 DOI: 10.1021/acs.jmedchem.4c00627 |
0.369 |
|
| 2024 |
Distler K, Maschauer S, Neu E, Hübner H, Einsiedel J, Prante O, Gmeiner P. Structure-guided discovery of orexin receptor-binding PET ligands. Bioorganic & Medicinal Chemistry. 110: 117823. PMID 38964170 DOI: 10.1016/j.bmc.2024.117823 |
0.318 |
|
| 2024 |
Vogt H, Shinkwin P, Huber ME, Staffen N, Hübner H, Gmeiner P, Schiedel M, Weikert D. Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. Acs Pharmacology & Translational Science. 7: 1533-1545. PMID 38751637 DOI: 10.1021/acsptsci.4c00086 |
0.395 |
|
| 2024 |
Chen G, Staffen N, Wu Z, Xu X, Pan J, Inoue A, Shi T, Gmeiner P, Du Y, Xu J. Structural and functional characterization of the endogenous agonist for orphan receptor GPR3. Cell Research. PMID 38287118 DOI: 10.1038/s41422-023-00919-8 |
0.39 |
|
| 2023 |
Lahmy R, Hübner H, Lachmann D, Gmeiner P, König B. Development of Photoswitchable Tethered Ligands that Target the μ-Opioid Receptor. Chemmedchem. e202300228. PMID 37817331 DOI: 10.1002/cmdc.202300228 |
0.456 |
|
| 2023 |
Graßl F, Bock L, Huete-Huerta González Á, Schiller M, Gmeiner P, König J, Fromm MF, Hübner H, Heinrich MR. Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists. Journal of Medicinal Chemistry. PMID 37450764 DOI: 10.1021/acs.jmedchem.3c00537 |
0.604 |
|
| 2023 |
Saller J, List C, Hübner H, Gmeiner P, Clark T, Pischetsrieder M. Identification and quantification of kukoamine A and kukoamine B as novel μ-opioid receptor agonists in potato and other solanaceous plants. Food Chemistry. 427: 136637. PMID 37385059 DOI: 10.1016/j.foodchem.2023.136637 |
0.348 |
|
| 2023 |
Kühl T, Georgieva MG, Hübner H, Lazarova M, Vogel M, Haas B, Peeva MI, Balacheva AA, Bogdanov IP, Milella L, Ponticelli M, Garev T, Faraone I, Detcheva R, Minchev B, ... ... Gmeiner P, et al. Neurotensin(8-13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease. European Journal of Medicinal Chemistry. 254: 115386. PMID 37094450 DOI: 10.1016/j.ejmech.2023.115386 |
0.353 |
|
| 2023 |
Xu X, Shonberg J, Kaindl J, Clark MJ, Stößel A, Maul L, Mayer D, Hübner H, Hirata K, Venkatakrishnan AJ, Dror RO, Kobilka BK, Sunahara RK, Liu X, Gmeiner P. Constrained catecholamines gain βAR selectivity through allosteric effects on pocket dynamics. Nature Communications. 14: 2138. PMID 37059717 DOI: 10.1038/s41467-023-37808-y |
0.401 |
|
| 2023 |
Fierro F, Peri L, Hübner H, Tabor-Schkade A, Waterloo L, Löber S, Pfeiffer T, Weikert D, Dingjan T, Margulis E, Gmeiner P, Niv MY. Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands. Cellular and Molecular Life Sciences : Cmls. 80: 114. PMID 37012410 DOI: 10.1007/s00018-023-04765-0 |
0.407 |
|
| 2023 |
Panel N, Vo DD, Kahlous NA, Hübner H, Tiedt S, Matricon P, Pacalon J, Fleetwood O, Kampen S, Luttens A, Delemotte L, Kihlberg J, Gmeiner P, Carlsson J. Design of Drug Efficacy Guided by Free Energy Simulations of the β2-Adrenoceptor. Angewandte Chemie (International Ed. in English). e202218959. PMID 36914577 DOI: 10.1002/anie.202218959 |
0.369 |
|
| 2023 |
Waterloo L, Hübner H, Fierro F, Pfeiffer T, Brox R, Löber S, Weikert D, Niv MY, Gmeiner P. Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14. Journal of Medicinal Chemistry. 66: 3499-3521. PMID 36847646 DOI: 10.1021/acs.jmedchem.2c01997 |
0.369 |
|
| 2023 |
Xu J, Wang Q, Hübner H, Hu Y, Niu X, Wang H, Maeda S, Inoue A, Tao Y, Gmeiner P, Du Y, Jin C, Kobilka BK. Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature Communications. 14: 376. PMID 36690613 DOI: 10.1038/s41467-022-35726-z |
0.353 |
|
| 2022 |
Waterloo LAW, Löber S, Gmeiner P. The Bitter Taste Receptor TAS2R14 as a Drug Target. Chimia. 76: 418-424. PMID 38069713 DOI: 10.2533/chimia.2022.418 |
0.368 |
|
| 2022 |
Wenk D, Khan S, Ignatchenko V, Hübner H, Gmeiner P, Weikert D, Pischetsrieder M, Kislinger T. Phosphoproteomic Analysis of Dopamine D2 Receptor Signaling Reveals Interplay of G Protein- and β-Arrestin-Mediated Effects. Journal of Proteome Research. 22: 259-271. PMID 36508580 DOI: 10.1021/acs.jproteome.2c00707 |
0.39 |
|
| 2022 |
Köckenberger J, Fischer O, Konopa A, Bergwinkl S, Mühlich S, Gmeiner P, Kutta RJ, Hübner H, Keller M, Heinrich MR. Synthesis, Characterization, and Application of Muscarinergic M Receptor Ligands Linked to Fluorescent Dyes. Journal of Medicinal Chemistry. PMID 36484801 DOI: 10.1021/acs.jmedchem.2c01376 |
0.337 |
|
| 2022 |
Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, ... ... Gmeiner P, et al. Structure-based discovery of nonopioid analgesics acting through the α-adrenergic receptor. Science (New York, N.Y.). 377: eabn7065. PMID 36173843 DOI: 10.1126/science.abn7065 |
0.359 |
|
| 2022 |
Lahmy R, Hübner H, Schmidt MF, Lachmann D, Gmeiner P, König B. Photochromic Fentanyl Derivatives for Controlled µ-Opioid Receptor Activation. Chemistry (Weinheim An Der Bergstrasse, Germany). PMID 35899620 DOI: 10.1002/chem.202201515 |
0.373 |
|
| 2022 |
Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y. Activation and allosteric regulation of the orphan GPR88-Gi1 signaling complex. Nature Communications. 13: 2375. PMID 35501348 DOI: 10.1038/s41467-022-30081-5 |
0.315 |
|
| 2022 |
Einsiedel J, Schmidt MF, Hübner H, Gmeiner P. Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors. Bioorganic & Medicinal Chemistry. 61: 116720. PMID 35334449 DOI: 10.1016/j.bmc.2022.116720 |
0.403 |
|
| 2022 |
Xu J, Cao S, Hübner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y. Structural insights into ligand recognition, activation, and signaling of the α adrenergic receptor. Science Advances. 8: eabj5347. PMID 35245122 DOI: 10.1126/sciadv.abj5347 |
0.358 |
|
| 2021 |
Nagai R, Sugimachi A, Tanimoto Y, Suzuki KGN, Hayashi F, Weikert D, Gmeiner P, Kasai RS, Morigaki K. Functional Reconstitution of Dopamine D2 Receptor into a Supported Model Membrane in a Nanometric Confinement. Advanced Biology. e2100636. PMID 34761565 DOI: 10.1002/adbi.202100636 |
0.379 |
|
| 2021 |
Budzinski J, Maschauer S, Kobayashi H, Couvineau P, Vogt H, Gmeiner P, Roggenhofer A, Prante O, Bouvier M, Weikert D. Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer. Communications Biology. 4: 1062. PMID 34508168 DOI: 10.1038/s42003-021-02574-4 |
0.542 |
|
| 2021 |
Boritzki V, Hübner H, Allikalt A, Gmeiner P, Wöhrl BM. Optimizing the Expression of Human Dopamine Receptors in . International Journal of Molecular Sciences. 22. PMID 34445358 DOI: 10.3390/ijms22168647 |
0.517 |
|
| 2021 |
Tropmann K, Bresinsky M, Forster L, Mönnich D, Buschauer A, Wittmann HJ, Hübner H, Gmeiner P, Pockes S, Strasser A. Abolishing Dopamine D/D Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H Receptor Agonists. Journal of Medicinal Chemistry. 64: 8684-8709. PMID 34110814 DOI: 10.1021/acs.jmedchem.1c00692 |
0.584 |
|
| 2021 |
Wenk D, Ignatchenko V, Macklin A, Hübner H, Gmeiner P, Weikert D, Pischetsrieder M, Kislinger T. Functionally selective activation of the dopamine receptor D is mirrored by the protein expression profiles. Scientific Reports. 11: 3501. PMID 33568753 DOI: 10.1038/s41598-021-83038-x |
0.432 |
|
| 2021 |
Voyer D, Einsiedel J, Gmeiner P, Lévesque D, Rompré PP. Sensitization to amphetamine psychostimulant effect: A key role for ventral tegmental area neurotensin type 2 receptors and MAP kinase pathway. Addiction Biology. e13008. PMID 33491227 DOI: 10.1111/adb.13008 |
0.441 |
|
| 2021 |
Ullmann T, Gienger M, Budzinski J, Hellmann J, Hübner H, Gmeiner P, Weikert D. Homobivalent Dopamine D Receptor Ligands Modulate the Dynamic Equilibrium of D Monomers and Homo- and Heterodimers. Acs Chemical Biology. PMID 33435665 DOI: 10.1021/acschembio.0c00895 |
0.523 |
|
| 2020 |
Allikalt A, Purkayastha N, Flad K, Schmidt MF, Tabor A, Gmeiner P, Hübner H, Weikert D. Fluorescent ligands for dopamine D/D receptors. Scientific Reports. 10: 21842. PMID 33318558 DOI: 10.1038/s41598-020-78827-9 |
0.496 |
|
| 2020 |
Uzuneser TC, Weiss EM, Dahlmanns J, Kalinichenko LS, Amato D, Kornhuber J, Alzheimer C, Hellmann J, Kaindl J, Hübner H, Löber S, Gmeiner P, Grömer TW, Müller CP. Presynaptic vesicular accumulation is required for antipsychotic efficacy in psychotic-like rats. Journal of Psychopharmacology (Oxford, England). 269881120965908. PMID 33274688 DOI: 10.1177/0269881120965908 |
0.324 |
|
| 2020 |
Xu X, Kaindl J, Clark MJ, Hübner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X. Binding pathway determines norepinephrine selectivity for the human βAR over βAR. Cell Research. PMID 33093660 DOI: 10.1038/s41422-020-00424-2 |
0.357 |
|
| 2020 |
Willmann M, Ermert J, Prante O, Hübner H, Gmeiner P, Neumaier B. Radiosynthesis and evaluation of F-labeled dopamine D-receptor ligands. Nuclear Medicine and Biology. PMID 32718750 DOI: 10.1016/j.nucmedbio.2020.07.004 |
0.521 |
|
| 2020 |
Hellmann J, Drabek M, Yin J, Gunera J, Pröll T, Kraus F, Langmead CJ, Hübner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P. Structure-based development of a subtype-selective orexin 1 receptor antagonist. Proceedings of the National Academy of Sciences of the United States of America. PMID 32669442 DOI: 10.1073/Pnas.2002704117 |
0.411 |
|
| 2020 |
Klösel I, Schmidt MF, Kaindl J, Hübner H, Weikert D, Gmeiner P. Discovery of Novel Nonpeptidic PAR2 Ligands. Acs Medicinal Chemistry Letters. 11: 1316-1323. PMID 32551018 DOI: 10.1021/acsmedchemlett.0c00154 |
0.369 |
|
| 2020 |
Liu X, Kaindl J, Korczynska M, Stößel A, Dengler D, Stanek M, Hübner H, Clark MJ, Mahoney J, Matt RA, Xu X, Hirata K, Shoichet BK, Sunahara RK, Kobilka BK, ... Gmeiner P, et al. An allosteric modulator binds to a conformational hub in the β adrenergic receptor. Nature Chemical Biology. PMID 32483378 DOI: 10.1038/S41589-020-0549-2 |
0.389 |
|
| 2020 |
Krüll J, Fehler SK, Hofmann L, Nebel N, Maschauer S, Prante O, Gmeiner P, Lanig H, Hübner H, Heinrich MR. Synthesis, Radiosynthesis and Biological Evaluation of Buprenorphine-Derived Phenylazocarboxamides as Novel μ-Opioid Receptor Ligands. Chemmedchem. 15: 1175-1186. PMID 32378310 DOI: 10.1002/cmdc.202000180 |
0.435 |
|
| 2020 |
Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK. Activation of the α adrenoceptor by the sedative sympatholytic dexmedetomidine. Nature Chemical Biology. PMID 32152538 DOI: 10.1038/S41589-020-0492-2 |
0.352 |
|
| 2020 |
Stolwijk JA, Mildner AK, Kade C, Skiba M, Bernhardt G, Buschauer A, Huebner H, Gmeiner P, Wegener J. Stepwise Dosing Protocol for Increased Throughput in Label-Free Impedance-Based GPCR Assays. Journal of Visualized Experiments : Jove. PMID 32150162 DOI: 10.3791/60686 |
0.325 |
|
| 2020 |
Gienger M, Hübner H, Löber S, König B, Gmeiner P. Structure-based development of caged dopamine D/D receptor antagonists. Scientific Reports. 10: 829. PMID 31965029 DOI: 10.1038/S41598-020-57770-9 |
0.602 |
|
| 2020 |
Di Pizio A, Waterloo LAW, Brox R, Löber S, Weikert D, Behrens M, Gmeiner P, Niv MY. Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back. Cellular and Molecular Life Sciences : Cmls. 77: 531-542. PMID 31236627 DOI: 10.1007/s00018-019-03194-2 |
0.408 |
|
| 2019 |
Plach M, Schäfer T, Borroto-Escuela DO, Weikert D, Gmeiner P, Fuxe K, Friedland K. Differential allosteric modulation within dopamine DR - neurotensin NTS1R and DR - serotonin 5-HTR receptor complexes gives bias to intracellular calcium signalling. Scientific Reports. 9: 16312. PMID 31704949 DOI: 10.1038/S41598-019-52540-8 |
0.436 |
|
| 2019 |
Pirzer AS, Lasch R, Friedrich H, Hübner H, Gmeiner P, Heinrich MR. Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D Receptor Agonists with High Subtype Selectivity. Journal of Medicinal Chemistry. 62: 9658-9679. PMID 31613617 DOI: 10.1021/acs.jmedchem.9b01085 |
0.633 |
|
| 2019 |
Kling RC, Burchardt C, Einsiedel J, Hübner H, Gmeiner P. Structure-based exploration of an allosteric binding pocket in the NTS1 receptor using bitopic NT(8-13) derivatives and molecular dynamics simulations. Journal of Molecular Modeling. 25: 193. PMID 31209646 DOI: 10.1007/s00894-019-4064-x |
0.366 |
|
| 2019 |
Schwalbe T, Huebner H, Gmeiner P. Development of covalent antagonists for β1- and β2-adrenergic receptors. Bioorganic & Medicinal Chemistry. 27: 2959-2971. PMID 31151791 DOI: 10.1016/j.bmc.2019.05.034 |
0.389 |
|
| 2019 |
Xu J, Hu Y, Kaindl J, Risel P, Hübner H, Maeda S, Niu X, Li H, Gmeiner P, Jin C, Kobilka BK. Conformational Complexity and Dynamics in a Muscarinic Receptor Revealed by NMR Spectroscopy. Molecular Cell. PMID 31103421 DOI: 10.1016/J.Molcel.2019.04.028 |
0.351 |
|
| 2019 |
Stolwijk JA, Skiba M, Kade C, Bernhardt G, Buschauer A, Hübner H, Gmeiner P, Wegener J. Increasing the throughput of label-free cell assays to study the activation of G-protein-coupled receptors by using a serial agonist exposure protocol. Integrative Biology : Quantitative Biosciences From Nano to Macro. PMID 31083709 DOI: 10.1093/intbio/zyz010 |
0.34 |
|
| 2019 |
Stanek M, Picard LP, Schmidt MF, Kaindl JM, Hübner H, Bouvier M, Weikert D, Gmeiner P. Hybridization of β-adrenergic agonists and antagonists confers G protein bias. Journal of Medicinal Chemistry. PMID 31042379 DOI: 10.1021/Acs.Jmedchem.9B00349 |
0.303 |
|
| 2019 |
Sommer T, Dlugash G, Hübner H, Gmeiner P, Pischetsrieder M. Monitoring of the dopamine D2 receptor agonists hordenine and N-methyltyramine during the brewing process and in commercial beer samples. Food Chemistry. 276: 745-753. PMID 30409657 DOI: 10.1016/j.foodchem.2018.10.067 |
0.482 |
|
| 2018 |
Liu H, Hofmann J, Fish I, Schaake B, Eitel K, Bartuschat A, Kaindl J, Rampp H, Banerjee A, Hübner H, Clark MJ, Vincent SG, Fisher JT, Heinrich MR, Hirata K, ... ... Gmeiner P, et al. Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists. Proceedings of the National Academy of Sciences of the United States of America. PMID 30404914 DOI: 10.1073/Pnas.1813988115 |
0.313 |
|
| 2017 |
She X, Pegoli A, Mayr J, Hübner H, Bernhardt G, Gmeiner P, Keller M. Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased MR Affinity and Selectivity. Acs Omega. 2: 6741-6754. PMID 30023530 DOI: 10.1021/acsomega.7b01085 |
0.338 |
|
| 2017 |
Nebel N, Strauch B, Maschauer S, Lasch R, Rampp H, Fehler SK, Bock LR, Hübner H, Gmeiner P, Heinrich MR, Prante O. [F]Fluorophenylazocarboxylates: Design and Synthesis of Potential Radioligands for Dopamine D3 and μ-Opioid Receptor. Acs Omega. 2: 8649-8659. PMID 29479577 DOI: 10.1021/acsomega.7b01374 |
0.395 |
|
| 2017 |
Fish I, Stoessel A, Eitel K, Valant C, Albold S, Hübner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P. Structure-based design and discovery of new M2 receptor agonists. Journal of Medicinal Chemistry. PMID 29094937 DOI: 10.1021/Acs.Jmedchem.7B01113 |
0.411 |
|
| 2017 |
Tabor A, Möller D, Hübner H, Kornhuber J, Gmeiner P. Visualization of ligand-induced dopamine D and D receptor internalization by TIRF microscopy. Scientific Reports. 7: 10894. PMID 28883522 DOI: 10.1038/S41598-017-11436-1 |
0.498 |
|
| 2017 |
Männel B, Hübner H, Möller D, Gmeiner P. β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. Bioorganic & Medicinal Chemistry. 25: 5613-5628. PMID 28870802 DOI: 10.1016/j.bmc.2017.08.037 |
0.534 |
|
| 2017 |
Männel B, Jaiteh M, Zeifman A, Randakova A, Möller D, Hübner H, Gmeiner P, Carlsson J. Structure-Guided Screening for Functionally Selective DDopamine Receptor Ligands from a Virtual Chemical Library. Acs Chemical Biology. 12: 2652-2661. PMID 28846380 DOI: 10.1021/Acschembio.7B00493 |
0.412 |
|
| 2017 |
Schwalbe T, Kaindl J, Hübner H, Gmeiner P. Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. Bioorganic & Medicinal Chemistry. 25: 5084-5094. PMID 28666858 DOI: 10.1016/j.bmc.2017.06.034 |
0.598 |
|
| 2017 |
Lachmann D, Studte C, Männel B, Hübner H, Gmeiner P, König B. Photochromic Dopamine Receptor Ligands Based on Dithienylethenes and Fulgides. Chemistry (Weinheim An Der Bergstrasse, Germany). 23: 13423-13434. PMID 28650111 DOI: 10.1002/Chem.201702147 |
0.482 |
|
| 2017 |
Stößel A, Brox R, Purkayastha N, Hübner H, Hocke C, Prante O, Gmeiner P. Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior. Bioorganic & Medicinal Chemistry. PMID 28495386 DOI: 10.1016/j.bmc.2017.04.036 |
0.498 |
|
| 2017 |
Männel B, Dengler D, Shonberg J, Hübner H, Möller D, Gmeiner P. Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased DR Agonists. Journal of Medicinal Chemistry. 60: 4693-4713. PMID 28489379 DOI: 10.1021/acs.jmedchem.7b00363 |
0.456 |
|
| 2017 |
Pegoli A, She X, Wifling D, Hübner H, Bernhardt G, Gmeiner P, Keller M. Radiolabeled dibenzodiazepinone-type antagonists give evidence of dualsteric binding at the M2 muscarinic acetylcholine receptor. Journal of Medicinal Chemistry. PMID 28388054 DOI: 10.1021/acs.jmedchem.6b01892 |
0.324 |
|
| 2017 |
Sommer T, Hübner H, El Kerdawy A, Gmeiner P, Pischetsrieder M, Clark T. Identification of the Beer Component Hordenine as Food-Derived Dopamine D2 Receptor Agonist by Virtual Screening a 3D Compound Database. Scientific Reports. 7: 44201. PMID 28281694 DOI: 10.1038/Srep44201 |
0.386 |
|
| 2017 |
Möller D, Banerjee A, Uzuneser TC, Skultety M, Huth T, Plouffe B, Hübner H, Alzheimer C, Friedland K, Müller CP, Bouvier M, Gmeiner P. Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. Journal of Medicinal Chemistry. PMID 28248104 DOI: 10.1021/Acs.Jmedchem.6B01857 |
0.543 |
|
| 2016 |
Naporra F, Gobleder S, Wittmann HJ, Spindler J, Bodensteiner M, Bernhardt G, Hübner H, Gmeiner P, Elz S, Strasser A. Dibenzo[b,f][1,4]oxazepines and dibenzo[b,e]oxepines: Influence of the chlorine substitution pattern on the pharmacology at the HR, HR, 5-HTR and other selected GPCRs. Pharmacological Research. 113: 610-625. PMID 27697645 DOI: 10.1016/j.phrs.2016.09.042 |
0.373 |
|
| 2016 |
Tabor A, Weisenburger S, Banerjee A, Purkayastha N, Kaindl JM, Hübner H, Wei L, Grömer TW, Kornhuber J, Tschammer N, Birdsall NJ, Mashanov GI, Sandoghdar V, Gmeiner P. Visualization and ligand-induced modulation of dopamine receptor dimerization at the single molecule level. Scientific Reports. 6: 33233. PMID 27615810 DOI: 10.1038/Srep33233 |
0.809 |
|
| 2016 |
Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, ... ... Gmeiner P, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 1-6. PMID 27533032 DOI: 10.1038/Nature19112 |
0.741 |
|
| 2016 |
Hübner H, Schellhorn T, Gienger M, Schaab C, Kaindl J, Leeb L, Clark T, Möller D, Gmeiner P. Structure-guided development of heterodimer-selective GPCR ligands. Nature Communications. 7: 12298. PMID 27457610 DOI: 10.1038/Ncomms12298 |
0.48 |
|
| 2016 |
Weichert D, Stanek M, Hübner H, Gmeiner P. Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. Bioorganic & Medicinal Chemistry. 24: 2641-53. PMID 27132867 DOI: 10.1016/j.bmc.2016.04.028 |
0.555 |
|
| 2016 |
Kling RC, Plomer M, Lang C, Banerjee A, Hübner H, Gmeiner P. Development of Covalent Ligand-Receptor Pairs to Study the Binding Properties of Nonpeptidic Neurotensin Receptor 1 Antagonists. Acs Chemical Biology. PMID 26808719 DOI: 10.1021/acschembio.5b00965 |
0.445 |
|
| 2016 |
Kling RC, Clark T, Gmeiner P. Comparative MD Simulations Indicate a Dual Role for Arg1323.50 in Dopamine-Dependent D2R Activation. Plos One. 11: e0146612. PMID 26741139 DOI: 10.1371/Journal.Pone.0146612 |
0.47 |
|
| 2016 |
Nebel N, Maschauer S, Hocke C, Hübner H, Gmeiner P, Prante O. Optimization and synthesis of an (18) F-labeled dopamine D3 receptor ligand using [(18) F]fluorophenylazocarboxylic tert-butylester. Journal of Labelled Compounds & Radiopharmaceuticals. 59: 48-53. PMID 26707848 DOI: 10.1002/jlcr.3361 |
0.491 |
|
| 2015 |
Möller D, Salama I, Kling RC, Hübner H, Gmeiner P. 1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation. Bioorganic & Medicinal Chemistry. 23: 6195-209. PMID 26299826 DOI: 10.1016/j.bmc.2015.07.050 |
0.616 |
|
| 2015 |
Stucchi M, Gmeiner P, Huebner H, Rainoldi G, Sacchetti A, Silvani A, Lesma G. Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library. Acs Medicinal Chemistry Letters. 6: 882-7. PMID 26288260 DOI: 10.1021/acsmedchemlett.5b00131 |
0.622 |
|
| 2015 |
Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, et al. Structural insights into µ-opioid receptor activation. Nature. 524: 315-21. PMID 26245379 DOI: 10.1038/Nature14886 |
0.422 |
|
| 2015 |
Weichert D, Gmeiner P. Covalent molecular probes for class A G protein-coupled receptors: advances and applications. Acs Chemical Biology. 10: 1376-86. PMID 25860503 DOI: 10.1021/acschembio.5b00070 |
0.377 |
|
| 2015 |
Weichert D, Banerjee A, Hiller C, Kling RC, Hübner H, Gmeiner P. Molecular determinants of biased agonism at the dopamine D₂ receptor. Journal of Medicinal Chemistry. 58: 2703-17. PMID 25734236 DOI: 10.1021/jm501889t |
0.546 |
|
| 2015 |
Shonberg J, Kling RC, Gmeiner P, Löber S. GPCR crystal structures: Medicinal chemistry in the pocket. Bioorganic & Medicinal Chemistry. 23: 3880-906. PMID 25638496 DOI: 10.1016/j.bmc.2014.12.034 |
0.431 |
|
| 2015 |
Bartuschat AL, Schellhorn T, Hübner H, Gmeiner P, Heinrich MR. Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. Bioorganic & Medicinal Chemistry. 23: 3938-47. PMID 25564378 DOI: 10.1016/j.bmc.2014.12.012 |
0.546 |
|
| 2014 |
Schaab C, Kling RC, Einsiedel J, Hübner H, Clark T, Seebach D, Gmeiner P. Structure-based evolution of subtype-selective neurotensin receptor ligands. Chemistryopen. 3: 206-18. PMID 25478316 DOI: 10.1002/Open.201402031 |
0.423 |
|
| 2014 |
Nebel N, Maschauer S, Bartuschat AL, Fehler SK, Hübner H, Gmeiner P, Kuwert T, Heinrich MR, Prante O, Hocke C. Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging. Bioorganic & Medicinal Chemistry Letters. 24: 5399-403. PMID 25453796 DOI: 10.1016/j.bmcl.2014.10.043 |
0.537 |
|
| 2014 |
Salama I, Löber S, Hübner H, Gmeiner P. Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors. Bioorganic & Medicinal Chemistry Letters. 24: 3753-6. PMID 25047579 DOI: 10.1016/j.bmcl.2014.06.079 |
0.602 |
|
| 2014 |
Weichert D, Kruse AC, Manglik A, Hiller C, Zhang C, Hübner H, Kobilka BK, Gmeiner P. Covalent agonists for studying G protein-coupled receptor activation. Proceedings of the National Academy of Sciences of the United States of America. 111: 10744-8. PMID 25006259 DOI: 10.1073/Pnas.1410415111 |
0.483 |
|
| 2014 |
Kling RC, Tschammer N, Lanig H, Clark T, Gmeiner P. Active-state model of a dopamine D2 receptor-Gαi complex stabilized by aripiprazole-type partial agonists. Plos One. 9: e100069. PMID 24932547 DOI: 10.1371/Journal.Pone.0100069 |
0.788 |
|
| 2014 |
Möller D, Kling RC, Skultety M, Leuner K, Hübner H, Gmeiner P. Functionally selective dopamine D2, D3 receptor partial agonists Journal of Medicinal Chemistry. 57: 4861-4875. PMID 24831693 DOI: 10.1021/jm5004039 |
0.566 |
|
| 2014 |
Hocke C, Cumming P, Maschauer S, Kuwert T, Gmeiner P, Prante O. Biodistribution studies of two 18F-labeled pyridinylphenyl amides as subtype selective radioligands for the dopamine D3 receptor. Nuclear Medicine and Biology. 41: 223-8. PMID 24480780 DOI: 10.1016/J.Nucmedbio.2013.12.014 |
0.376 |
|
| 2014 |
Fehler SK, Maschauer S, Höfling SB, Bartuschat AL, Tschammer N, Hübner H, Gmeiner P, Prante O, Heinrich MR. Fast and efficient (18) F-labeling by [(18) f]fluorophenylazocarboxylic esters. Chemistry (Weinheim An Der Bergstrasse, Germany). 20: 370-5. PMID 24339325 DOI: 10.1002/chem.201303409 |
0.611 |
|
| 2014 |
Lang C, Gmeiner P. ChemInform Abstract: Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation. Cheminform. 45: no-no. DOI: 10.1002/CHIN.201405037 |
0.389 |
|
| 2013 |
Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 504: 101-6. PMID 24256733 DOI: 10.1038/Nature12735 |
0.414 |
|
| 2013 |
Banerjee A, Maschauer S, Hübner H, Gmeiner P, Prante O. Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers. Bioorganic & Medicinal Chemistry Letters. 23: 6079-82. PMID 24100078 DOI: 10.1016/j.bmcl.2013.09.026 |
0.611 |
|
| 2013 |
Kruse AC, Weiss DR, Rossi M, Hu J, Hu K, Eitel K, Gmeiner P, Wess J, Kobilka BK, Shoichet BK. Muscarinic receptors as model targets and antitargets for structure-based ligand discovery. Molecular Pharmacology. 84: 528-40. PMID 23887926 DOI: 10.1124/Mol.113.087551 |
0.41 |
|
| 2013 |
Jantschak F, Brosda J, Franke RT, Fink H, Möller D, Hübner H, Gmeiner P, Pertz HH. Pharmacological profile of 2-bromoterguride at human dopamine D 2, porcine serotonin 5-hydroxytryptamine 2A, and α 2C-adrenergic receptors, and its antipsychotic-like effects in rats Journal of Pharmacology and Experimental Therapeutics. 347: 57-68. PMID 23863695 DOI: 10.1124/jpet.113.205997 |
0.553 |
|
| 2013 |
Kling RC, Lanig H, Clark T, Gmeiner P. Active-state models of ternary GPCR complexes: determinants of selective receptor-G-protein coupling. Plos One. 8: e67244. PMID 23826246 DOI: 10.1371/Journal.Pone.0067244 |
0.346 |
|
| 2013 |
Hiller C, Kling RC, Heinemann FW, Meyer K, Hübner H, Gmeiner P. Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. Journal of Medicinal Chemistry. 56: 5130-41. PMID 23730937 DOI: 10.1021/Jm400520C |
0.456 |
|
| 2013 |
Hiller C, Kühhorn J, Gmeiner P. Class A G-protein-coupled receptor (GPCR) dimers and bivalent ligands. Journal of Medicinal Chemistry. 56: 6542-59. PMID 23678887 DOI: 10.1021/jm4004335 |
0.332 |
|
| 2013 |
Sanna F, Corda MG, Melis MR, Piludu MA, Löber S, Hübner H, Gmeiner P, Argiolas A, Giorgi O. Dopamine agonist-induced penile erection and yawning: a comparative study in outbred Roman high- and low-avoidance rats. Pharmacology, Biochemistry, and Behavior. 109: 59-66. PMID 23664901 DOI: 10.1016/j.pbb.2013.05.002 |
0.397 |
|
| 2013 |
Held C, Hübner H, Kling R, Nagel YA, Wennemers H, Gmeiner P. Impact of the proline residue on ligand binding of neurotensin receptor 2 (NTS2)-selective peptide-peptoid hybrids. Chemmedchem. 8: 772-8. PMID 23532897 DOI: 10.1002/Cmdc.201300054 |
0.4 |
|
| 2013 |
Sanna F, Ortner B, Hübner H, Löber S, Tschammer N, Gmeiner P. Discovery of dopamine D₄ receptor antagonists with planar chirality. Bioorganic & Medicinal Chemistry. 21: 1680-4. PMID 23428965 DOI: 10.1016/j.bmc.2013.01.065 |
0.815 |
|
| 2013 |
Held C, Plomer M, Hübner H, Meltretter J, Pischetsrieder M, Gmeiner P. Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand. Chemmedchem. 8: 75-81. PMID 23097347 DOI: 10.1002/cmdc.201200376 |
0.401 |
|
| 2013 |
Gmeiner P, Lang C. Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation Synthesis. 45: 2474-2480. DOI: 10.1055/S-0033-1338497 |
0.39 |
|
| 2012 |
Löber S, Hübner H, Buschauer A, Sanna F, Argiolas A, Melis MR, Gmeiner P. Novel azulene derivatives for the treatment of erectile dysfunction. Bioorganic & Medicinal Chemistry Letters. 22: 7151-4. PMID 23099096 DOI: 10.1016/j.bmcl.2012.09.064 |
0.551 |
|
| 2012 |
Trincavelli ML, Daniele S, Orlandini E, Navarro G, Casadó V, Giacomelli C, Nencetti S, Nuti E, Macchia M, Huebner H, Gmeiner P, Rossello A, Lluís C, Martini C. A new D₂ dopamine receptor agonist allosterically modulates A(2A) adenosine receptor signalling by interacting with the A(2A)/D₂ receptor heteromer. Cellular Signalling. 24: 951-60. PMID 22230688 DOI: 10.1016/j.cellsig.2011.12.018 |
0.385 |
|
| 2012 |
Koschatzky S, Gmeiner P. Selective agonists for dopamine/neurotensin receptor heterodimers. Chemmedchem. 7: 509-14. PMID 22213714 DOI: 10.1002/cmdc.201100499 |
0.589 |
|
| 2012 |
Huber D, Löber S, Hübner H, Gmeiner P. Bivalent molecular probes for dopamine D2-like receptors. Bioorganic & Medicinal Chemistry. 20: 455-66. PMID 22100258 DOI: 10.1016/j.bmc.2011.10.063 |
0.622 |
|
| 2011 |
Koschatzky S, Tschammer N, Gmeiner P. Cross-receptor interactions between dopamine D2L and neurotensin NTS1 receptors modulate binding affinities of dopaminergics. Acs Chemical Neuroscience. 2: 308-16. PMID 22778874 DOI: 10.1021/cn200020y |
0.813 |
|
| 2011 |
Kügler F, Sihver W, Ermert J, Hübner H, Gmeiner P, Prante O, Coenen HH. Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding. Journal of Medicinal Chemistry. 54: 8343-52. PMID 22039961 DOI: 10.1021/jm200762g |
0.518 |
|
| 2011 |
Goetz A, Lanig H, Gmeiner P, Clark T. Molecular dynamics simulations of the effect of the G-protein and diffusible ligands on the β2-adrenergic receptor. Journal of Molecular Biology. 414: 611-23. PMID 22037586 DOI: 10.1016/J.Jmb.2011.10.015 |
0.428 |
|
| 2011 |
Kühhorn J, Götz A, Hübner H, Thompson D, Whistler J, Gmeiner P. Development of a bivalent dopamine D₂ receptor agonist. Journal of Medicinal Chemistry. 54: 7911-9. PMID 21999579 DOI: 10.1021/Jm2009919 |
0.625 |
|
| 2011 |
Sanna F, Succu S, Hübner H, Gmeiner P, Argiolas A, Melis MR. 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. Behavioural Brain Research. 225: 169-76. PMID 21784104 DOI: 10.1016/j.bbr.2011.07.018 |
0.544 |
|
| 2011 |
Kühhorn J, Hübner H, Gmeiner P. Bivalent dopamine D2 receptor ligands: synthesis and binding properties. Journal of Medicinal Chemistry. 54: 4896-903. PMID 21599022 DOI: 10.1021/jm2004859 |
0.541 |
|
| 2011 |
Pratsch G, Unfried JF, Einsiedel J, Plomer M, Hübner H, Gmeiner P, Heinrich MR. Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand. Organic & Biomolecular Chemistry. 9: 3746-52. PMID 21472182 DOI: 10.1039/c1ob05292f |
0.426 |
|
| 2011 |
Einsiedel J, Held C, Hervet M, Plomer M, Tschammer N, Hübner H, Gmeiner P. Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics. Journal of Medicinal Chemistry. 54: 2915-23. PMID 21446649 DOI: 10.1021/jm200006c |
0.746 |
|
| 2011 |
Tschammer N, Elsner J, Goetz A, Ehrlich K, Schuster S, Ruberg M, Kühhorn J, Thompson D, Whistler J, Hübner H, Gmeiner P. Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions. Journal of Medicinal Chemistry. 54: 2477-91. PMID 21388142 DOI: 10.1021/Jm101639T |
0.817 |
|
| 2011 |
Löber S, Hübner H, Tschammer N, Gmeiner P. Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Trends in Pharmacological Sciences. 32: 148-57. PMID 21232805 DOI: 10.1016/j.tips.2010.12.003 |
0.786 |
|
| 2011 |
Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, Rasmussen SG, Choi HJ, Devree BT, Sunahara RK, Chae PS, Gellman SH, Dror RO, Shaw DE, Weis WI, ... ... Gmeiner P, et al. Structure and function of an irreversible agonist-β(2) adrenoceptor complex. Nature. 469: 236-40. PMID 21228876 DOI: 10.1038/Nature09665 |
0.404 |
|
| 2011 |
Tschammer N, Bollinger S, Kenakin T, Gmeiner P. Histidine 6.55 is a major determinant of ligand-biased signaling in dopamine D2L receptor. Molecular Pharmacology. 79: 575-85. PMID 21163968 DOI: 10.1124/mol.110.068106 |
0.782 |
|
| 2010 |
Tschammer N, Dörfler M, Hübner H, Gmeiner P. Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine. Acs Chemical Neuroscience. 1: 25-35. PMID 22778805 DOI: 10.1021/cn900001b |
0.806 |
|
| 2010 |
Ortega R, Hübner H, Gmeiner P, Masaguer CF. Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands. Bioorganic & Medicinal Chemistry Letters. 21: 2670-4. PMID 21273071 DOI: 10.1016/j.bmcl.2010.12.083 |
0.645 |
|
| 2010 |
Höfling SB, Maschauer S, Hübner H, Gmeiner P, Wester HJ, Prante O, Heinrich MR. Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET. Bioorganic & Medicinal Chemistry Letters. 20: 6933-7. PMID 21030255 DOI: 10.1016/j.bmcl.2010.09.142 |
0.374 |
|
| 2010 |
Bollinger S, Hübner H, Heinemann FW, Meyer K, Gmeiner P. Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. Journal of Medicinal Chemistry. 53: 7167-79. PMID 20860381 DOI: 10.1021/Jm100835Q |
0.311 |
|
| 2010 |
Skultety M, Hübner H, Löber S, Gmeiner P. Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors. Journal of Medicinal Chemistry. 53: 7219-28. PMID 20839776 DOI: 10.1021/jm100899z |
0.508 |
|
| 2010 |
Hocke C, Maschauer S, Hübner H, Löber S, Utz W, Kuwert T, Gmeiner P, Prante O. A series of 18F-labelled pyridinylphenyl amides as subtype-selective radioligands for the dopamine D3 receptor. Chemmedchem. 5: 941-8. PMID 20408162 DOI: 10.1002/cmdc.201000067 |
0.449 |
|
| 2010 |
Loeber S, Huebner H, Gmeiner P. ChemInform Abstract: Fused Azaindole Derivatives: Molecular Design, Synthesis and in vitro Pharmacology Leading to the Preferential Dopamine D3 Receptor Agonist FAUC 725. Cheminform. 33: no-no. DOI: 10.1002/CHIN.200251155 |
0.548 |
|
| 2010 |
Bergauer M, Huebner H, Gmeiner P. ChemInform Abstract: 2,4-Disubstituted Pyrroles: Synthesis, Traceless Linking and Pharmacological Investigations Leading to the Dopamine D4 Receptor Partial Agonist FAUC 356. Cheminform. 33: no-no. DOI: 10.1002/CHIN.200243195 |
0.579 |
|
| 2010 |
Loeber S, Aboul-Fadl T, Huebner H, Gmeiner P. ChemInform Abstract: Di- and Trisubstituted Pyrazolo[1,5-a]pyridine Derivatives: Synthesis, Dopamine Receptor Binding and Ligand Efficacy. Cheminform. 33: no-no. DOI: 10.1002/CHIN.200225139 |
0.5 |
|
| 2010 |
Lehmann T, Huebner H, Gmeiner P. ChemInform Abstract: Dopaminergic 7-Aminotetrahydroindolizines: Ex-Chiral Pool Synthesis and Preferential D3 Receptor Binding. Cheminform. 33: no-no. DOI: 10.1002/CHIN.200208149 |
0.547 |
|
| 2010 |
Einsiedel J, Huebner H, Gmeiner P. ChemInform Abstract: Benzamide Bioisosteres Incorporating Dihydroheteroazole Substructures: EPC Synthesis and SAR Leading to a Selective Dopamine D4 Receptor Partial Agonist (FAUC 179). Cheminform. 33: no-no. DOI: 10.1002/CHIN.200205152 |
0.584 |
|
| 2010 |
Ortner B, Waibel R, Gmeiner P. ChemInform Abstract: Indoloparacyclophanes: Synthesis and Dopamine Receptor Binding of a Novel Arylbioisostere. Cheminform. 32: no-no. DOI: 10.1002/CHIN.200129126 |
0.485 |
|
| 2010 |
Haubmann C, Huebner H, Gmeiner P. ChemInform Abstract: Piperidinylpyrroles: Design, Synthesis, and Binding Properties of Novel and Selective Dopamine D4 Receptor Ligands. Cheminform. 31: no-no. DOI: 10.1002/CHIN.200008156 |
0.582 |
|
| 2010 |
Haubmann C, Huebner H, Gmeiner P. ChemInform Abstract: 2,2-Dicyanovinyl as a Nonaromatic Aryl Bioisostere: Synthesis, Binding Experiments, and SAR Studies of Highly Selective Dopamine D4 Receptor Ligands. Cheminform. 30: no-no. DOI: 10.1002/CHIN.199943280 |
0.598 |
|
| 2010 |
Thomas C, Huebner H, Gmeiner P. ChemInform Abstract: Enantio- and Diastereocontrolled Dopamine D1, D2, D3, and D4 Receptor Binding of N-(3-Pyrrolidinylmethyl)benzamides Synthesized from Aspartic Acid. Cheminform. 30: no-no. DOI: 10.1002/CHIN.199926215 |
0.517 |
|
| 2010 |
Loeber S, Huebner H, Gmeiner P. ChemInform Abstract: Azaindole Derivatives with High Affinity for the Dopamine D4 Receptor: Synthesis, Ligand Binding Studies and Comparison of Molecular Electrostatic Potential Maps. Cheminform. 30: no-no. DOI: 10.1002/CHIN.199919161 |
0.551 |
|
| 2010 |
GMEINER P, BOLLINGER B, LOTTER H. ChemInform Abstract: 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. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199641118 |
0.456 |
|
| 2010 |
GMEINER P, KAERTNER A, MIERAU J. ChemInform Abstract: Synthesis and Dopamine Receptor Binding Studies of Homochiral 8- Aminopyrido(1,2-a)indoles. Cheminform. 26: no-no. DOI: 10.1002/CHIN.199551185 |
0.484 |
|
| 2010 |
GMEINER P, BOLLINGER B, MIERAU J, HOEFNER G. ChemInform Abstract: Synthesis, Pharmacological Investigation and Computational Studies on a Tricyclic Ergoline Analogue with Selective Dopamine Autoreceptor Activity. Cheminform. 26: no-no. DOI: 10.1002/CHIN.199551129 |
0.326 |
|
| 2010 |
GMEINER P, SOMMER J, HOEFNER G. ChemInform Abstract: Synthesis and Dopamine Receptor Binding of 3-Phenylazepino(5,4,3-c,d) indole Derivatives. Cheminform. 26: no-no. DOI: 10.1002/CHIN.199536194 |
0.553 |
|
| 2010 |
GMEINER P, SOMMER J, MIERAU J, HOEFNER G. ChemInform Abstract: Dopamine Autoreceptor Agonists: Computational Studies, Synthesis and Biological Investigations. Cheminform. 26: no-no. DOI: 10.1002/CHIN.199507160 |
0.337 |
|
| 2010 |
GMEINER P, SOMMER J. ChemInform Abstract: Selective Dopamine D-2 Autoreceptor Agonists with 8-Azaindole Substructure: Synthesis and Theoretical Investigations. Cheminform. 25: no-no. DOI: 10.1002/CHIN.199448167 |
0.496 |
|
| 2009 |
Huber D, Hübner H, Gmeiner P. 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. Journal of Medicinal Chemistry. 52: 6860-70. PMID 19807103 DOI: 10.1021/jm901120h |
0.62 |
|
| 2009 |
Ehrlich K, Götz A, Bollinger S, Tschammer N, Bettinetti L, Härterich S, Hübner H, Lanig H, Gmeiner P. Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding. Journal of Medicinal Chemistry. 52: 4923-35. PMID 19606869 DOI: 10.1021/jm900690y |
0.785 |
|
| 2009 |
Loaiza PR, Löber S, Hübner H, Gmeiner P. Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker. Bioorganic & Medicinal Chemistry. 17: 5482-7. PMID 19592258 DOI: 10.1016/j.bmc.2009.06.041 |
0.416 |
|
| 2009 |
Linz S, Müller J, Hübner H, Gmeiner P, Troschütz R. Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. Bioorganic & Medicinal Chemistry. 17: 4448-58. PMID 19481941 DOI: 10.1016/j.bmc.2009.05.015 |
0.531 |
|
| 2009 |
Löber S, Tschammer N, Hübner H, Melis MR, Argiolas A, Gmeiner P. The azulene framework as a novel arene bioisostere: design of potent dopamine D4 receptor ligands inducing penile erection. Chemmedchem. 4: 325-8. PMID 19185034 DOI: 10.1002/cmdc.200800395 |
0.808 |
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| 2008 |
Dörfler M, Tschammer N, Hamperl K, Hübner H, Gmeiner P. Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. Journal of Medicinal Chemistry. 51: 6829-38. PMID 18834111 DOI: 10.1021/jm800895v |
0.8 |
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| 2008 |
Härterich S, Koschatzky S, Einsiedel J, Gmeiner P. Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1. Bioorganic & Medicinal Chemistry. 16: 9359-68. PMID 18809332 DOI: 10.1016/j.bmc.2008.08.051 |
0.417 |
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| 2008 |
Prante O, Tietze R, Hocke C, Löber S, Hübner H, Kuwert T, Gmeiner P. 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. Journal of Medicinal Chemistry. 51: 1800-10. PMID 18307287 DOI: 10.1021/jm701375u |
0.457 |
|
| 2008 |
Hocke C, Prante O, Salama I, Hübner H, Löber S, Kuwert T, Gmeiner P. 18F-Labeled FAUC 346 and BP 897 derivatives as subtype-selective potential PET radioligands for the dopamine D3 receptor. Chemmedchem. 3: 788-93. PMID 18306190 DOI: 10.1002/cmdc.200700327 |
0.528 |
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| 2008 |
Einsiedel J, Hübner H, Hervet M, Härterich S, Koschatzky S, Gmeiner P. Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. Bioorganic & Medicinal Chemistry Letters. 18: 2013-8. PMID 18276136 DOI: 10.1016/j.bmcl.2008.01.110 |
0.315 |
|
| 2008 |
Tietze R, Löber S, Hübner H, Gmeiner P, Kuwert T, Prante O. Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker. Bioorganic & Medicinal Chemistry Letters. 18: 983-8. PMID 18164618 DOI: 10.1016/j.bmcl.2007.12.026 |
0.424 |
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| 2007 |
Görnemann T, Hübner H, Gmeiner P, Horowski R, Latté KP, Flieger M, Pertz HH. Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors. The Journal of Pharmacology and Experimental Therapeutics. 324: 1136-45. PMID 18096760 DOI: 10.1124/jpet.107.133165 |
0.338 |
|
| 2007 |
Rodriguez Loaiza P, Löber S, Hübner H, Gmeiner P. Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. Bioorganic & Medicinal Chemistry. 15: 7248-57. PMID 17827018 DOI: 10.1016/J.BMC.2007.08.038 |
0.485 |
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| 2007 |
Stark D, Piel M, Hübner H, Gmeiner P, Gründer G, Rösch F. In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors. Bioorganic & Medicinal Chemistry. 15: 6819-29. PMID 17765546 DOI: 10.1016/j.bmc.2007.07.017 |
0.537 |
|
| 2007 |
Boeckler F, Gmeiner P. Dopamine D3 receptor ligands: recent advances in the control of subtype selectivity and intrinsic activity. Biochimica Et Biophysica Acta. 1768: 871-887. PMID 17274946 DOI: 10.1016/J.Bbamem.2006.12.001 |
0.839 |
|
| 2007 |
Salama I, Hocke C, Utz W, Prante O, Boeckler F, Hübner H, Kuwert T, Gmeiner P. Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands. Journal of Medicinal Chemistry. 50: 489-500. PMID 17266201 DOI: 10.1021/Jm0611152 |
0.82 |
|
| 2007 |
Gmeiner P. Laboratory Automation with Parallel Synthesis: A Solid Phase Supported Access to New Biogenic Amine Receptor Ligands Cheminform. 38. DOI: 10.1002/CHIN.200747238 |
0.315 |
|
| 2006 |
Melis MR, Succu S, Sanna F, Melis T, Mascia MS, Enguehard-Gueiffier C, Hubner H, Gmeiner P, Gueiffier A, Argiolas A. PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain. The European Journal of Neuroscience. 24: 2021-30. PMID 17067298 DOI: 10.1111/j.1460-9568.2006.05043.x |
0.445 |
|
| 2006 |
Boeckler F, Gmeiner P. The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects. Pharmacology & Therapeutics. 112: 281-333. PMID 16905195 DOI: 10.1016/J.Pharmthera.2006.04.007 |
0.825 |
|
| 2006 |
Enguehard-Gueiffier C, Hübner H, El Hakmaoui A, Allouchi H, Gmeiner P, Argiolas A, Melis MR, Gueiffier A. 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. Journal of Medicinal Chemistry. 49: 3938-47. PMID 16789750 DOI: 10.1021/jm060166w |
0.595 |
|
| 2006 |
Schlotter K, Boeckler F, Hübner H, Gmeiner P. Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. Journal of Medicinal Chemistry. 49: 3628-3635. PMID 16759104 DOI: 10.1021/Jm060138D |
0.833 |
|
| 2006 |
Salama I, Schlotter K, Utz W, Hübner H, Gmeiner P, Boeckler F. CoMFA and CoMSIA investigations of dopamine D3 receptor ligands leading to the prediction, synthesis, and evaluation of rigidized FAUC 365 analogues. Bioorganic & Medicinal Chemistry. 14: 5898-912. PMID 16750374 DOI: 10.1016/J.Bmc.2006.05.025 |
0.851 |
|
| 2006 |
Seeman P, Wilson A, Gmeiner P, Kapur S. Dopamine D2 and D3 receptors in human putamen, caudate nucleus, and globus pallidus. Synapse (New York, N.Y.). 60: 205-11. PMID 16739118 DOI: 10.1002/SYN.20298 |
0.56 |
|
| 2006 |
Löber S, Hübner H, Gmeiner P. Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. Bioorganic & Medicinal Chemistry Letters. 16: 2955-9. PMID 16563764 DOI: 10.1016/J.BMCL.2006.02.075 |
0.637 |
|
| 2006 |
Loaiza PR, Löber S, Hübner H, Gmeiner P. Click chemistry on solid phase: parallel synthesis of N-benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands. Journal of Combinatorial Chemistry. 8: 252-61. PMID 16529521 DOI: 10.1021/CC050127Q |
0.362 |
|
| 2006 |
Prante O, Hocke C, Löber S, Hübner H, Gmeiner P, Kuwert T. Tissue distribution of radioiodinated FAUC113: assessment of a pyrazolo(1,5-a) pyridine based dopamine D4 receptor radioligand candidate. Nuklearmedizin. Nuclear Medicine. 45: 41-8. PMID 16493513 DOI: 10.1267/NUKL06010041 |
0.513 |
|
| 2006 |
Elsner J, Boeckler F, Davidson K, Sugden D, Gmeiner P. Bicyclic melatonin receptor agonists containing a ring-junction nitrogen: Synthesis, biological evaluation, and molecular modeling of the putative bioactive conformation. Bioorganic & Medicinal Chemistry. 14: 1949-1958. PMID 16290939 DOI: 10.1016/J.Bmc.2005.10.042 |
0.781 |
|
| 2006 |
Bettinetti L, Löber S, Hübner H, Gmeiner P. Parallel synthesis and biological screening of dopamine receptor ligands taking advantage of a click chemistry based BAL linker. Journal of Combinatorial Chemistry. 7: 309-16. PMID 15762761 DOI: 10.1021/CC049860S |
0.567 |
|
| 2006 |
Hocke C, Löber S, Hübner H, Gmeiner P, Kuwert T, Prante O. Tissue distribution of radioiodinated FAUC113 Nuklearmedizin. 45: 41-48. DOI: 10.1055/s-0038-1623933 |
0.342 |
|
| 2006 |
Tietze R, Hocke C, Löber S, Hübner H, Kuwert T, Gmeiner P, Prante O. Syntheses and radiofluorination of two derivatives of 5-cyano-indole as selective ligands for the dopamine subtype-4 receptor Journal of Labelled Compounds and Radiopharmaceuticals. 49: 55-70. DOI: 10.1002/JLCR.1026 |
0.521 |
|
| 2006 |
Loeber S, Huebner H, Gmeiner P. Synthesis and Biological Investigations of Dopaminergic Partial Agonists Preferentially Recognizing the D4 Receptor Subtype. Cheminform. 37. DOI: 10.1002/CHIN.200635114 |
0.574 |
|
| 2005 |
Hocke C, Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T. Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents. Bioorganic & Medicinal Chemistry Letters. 15: 4819-23. PMID 16139501 DOI: 10.1016/J.BMCL.2005.07.037 |
0.502 |
|
| 2005 |
Elsner J, Boeckler F, Heinemann FW, Hübner H, Gmeiner P. Pharmacophore-Guided Drug Discovery Investigations Leading to Bioactive 5-Aminotetrahydropyrazolopyridines. Implications for the Binding Mode of Heterocyclic Dopamine D3 Receptor Agonists§ Journal of Medicinal Chemistry. 48: 5771-5779. PMID 16134944 DOI: 10.1021/Jm0503805 |
0.838 |
|
| 2005 |
Bettinetti L, Hübner H, Gmeiner P. Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs. Archiv Der Pharmazie. 338: 276-80. PMID 15952242 DOI: 10.1002/ARDP.200400997 |
0.403 |
|
| 2005 |
Schlotter K, Boeckler F, Hübner H, Gmeiner P. Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. Journal of Medicinal Chemistry. 48: 3696-3699. PMID 15916420 DOI: 10.1021/Jm050170S |
0.84 |
|
| 2005 |
Lenz C, Boeckler F, Hübner H, Gmeiner P. Fancy bioisosteres: Synthesis, SAR, and pharmacological investigations of novel nonaromatic dopamine D3 receptor ligands Bioorganic & Medicinal Chemistry. 13: 4434-4442. PMID 15908220 DOI: 10.1016/J.Bmc.2005.04.047 |
0.831 |
|
| 2005 |
Boeckler F, Ohnmacht U, Lehmann T, Utz W, Hübner H, Gmeiner P. CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. Journal of Medicinal Chemistry. 48: 2493-508. PMID 15801839 DOI: 10.1021/jm049269 |
0.851 |
|
| 2005 |
Boeckler F, Lanig H, Gmeiner P. Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes. Journal of Medicinal Chemistry. 48: 694-709. PMID 15689154 DOI: 10.1021/Jm049612A |
0.841 |
|
| 2005 |
Lenz C, Haubmann C, Hübner H, Boeckler F, Gmeiner P. Fancy bioisosteres: synthesis and dopaminergic properties of the endiyne FAUC 88 as a novel non-aromatic D3 agonist. Bioorganic & Medicinal Chemistry. 13: 185-191. PMID 15582463 DOI: 10.1016/J.Bmc.2004.09.044 |
0.833 |
|
| 2005 |
Hocke C, Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T. Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype. Bioorganic & Medicinal Chemistry Letters. 14: 3963-6. PMID 15225707 DOI: 10.1016/J.BMCL.2004.05.052 |
0.628 |
|
| 2004 |
Bittermann H, Einsiedel J, Hübner H, Gmeiner P. Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13). Journal of Medicinal Chemistry. 47: 5587-90. PMID 15481995 DOI: 10.1021/JM049644Y |
0.354 |
|
| 2004 |
Kortagere S, Gmeiner P, Weinstein H, Schetz JA. Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Molecular Pharmacology. 66: 1491-9. PMID 15448188 DOI: 10.1124/Mol.104.001321 |
0.561 |
|
| 2004 |
Hussenether T, Hübner H, Gmeiner P, Troschütz R. Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing. Bioorganic & Medicinal Chemistry. 12: 2625-37. PMID 15110844 DOI: 10.1016/J.BMC.2004.03.023 |
0.516 |
|
| 2004 |
Boeckler F, Russig H, Zhang W, Löber S, Schetz J, Hübner H, Ferger B, Gmeiner P, Feldon J. FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Psychopharmacology. 175: 7-17. PMID 15007532 DOI: 10.1007/S00213-004-1782-1 |
0.822 |
|
| 2004 |
Lenz C, Boeckler F, Hübner H, Gmeiner P. Analogues of FAUC 73 revealing new insights into the structural requirements of nonaromatic dopamine D3 receptor agonists Bioorganic & Medicinal Chemistry. 12: 113-117. PMID 14697776 DOI: 10.1016/J.Bmc.2003.10.011 |
0.825 |
|
| 2004 |
Einsiedel J, Weber K, Thomas C, Lehmann T, Hübner H, Gmeiner P. Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid. Bioorganic & Medicinal Chemistry Letters. 13: 3293-6. PMID 12951112 DOI: 10.1016/S0960-894X(03)00678-4 |
0.578 |
|
| 2004 |
Einsiedel J, Weber K, Thomas C, Lehmann T, Huebner H, Gmeiner P. Stereocontrolled Dopamine Receptor Binding and Subtype Selectivity of Clebopride Analogues Synthesized from Aspartic Acid. Cheminform. 35. DOI: 10.1002/CHIN.200401169 |
0.483 |
|
| 2003 |
Boeckler F, Leng A, Mura A, Bettinetti L, Feldon J, Gmeiner P, Ferger B. 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. Biochemical Pharmacology. 66: 1025-32. PMID 12963489 DOI: 10.1016/S0006-2952(03)00451-9 |
0.78 |
|
| 2003 |
Löber S, Rodriguez-Loaiza P, Gmeiner P. Click linker: efficient and high-yielding synthesis of a new family of SPOS resins by 1,3-dipolar cycloaddition. Organic Letters. 5: 1753-5. PMID 12735769 DOI: 10.1021/OL034520L |
0.372 |
|
| 2003 |
Einsiedel J, Hübner H, Gmeiner P. Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. Bioorganic & Medicinal Chemistry Letters. 13: 851-4. PMID 12617906 DOI: 10.1016/S0960-894X(03)00004-0 |
0.62 |
|
| 2003 |
Löber S, Hübner H, Gmeiner P. Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. Bioorganic & Medicinal Chemistry Letters. 12: 2377-80. PMID 12161137 DOI: 10.1016/S0960-894X(02)00390-6 |
0.58 |
|
| 2003 |
Bergauer M, Hübner H, Gmeiner P. 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. Bioorganic & Medicinal Chemistry Letters. 12: 1937-40. PMID 12113813 DOI: 10.1016/S0960-894X(02)00316-5 |
0.568 |
|
| 2003 |
Moll A, Hübner H, Gmeiner P, Troschütz R. Phenylpiperazinylmethylindolecarboxylates and derivatives as selective D(4)-ligands. Bioorganic & Medicinal Chemistry. 10: 1671-9. PMID 11937325 DOI: 10.1016/S0968-0896(02)00042-1 |
0.619 |
|
| 2003 |
Löber S, Aboul-Fadl T, Hübner H, Gmeiner P. Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. Bioorganic & Medicinal Chemistry Letters. 12: 633-6. PMID 11844688 DOI: 10.1016/S0960-894X(01)00814-9 |
0.56 |
|
| 2003 |
M. El-Abadelah M, Gmeiner P, Hübner H, A. Abu Safieh K, I. Fasfous I, S. Sabri S, Voelter W. Synthesis and Dopamine Receptor Binding of Some Pyrazolo[3’,4’:6,7]azepino[5,4,3-cd]indoles Heterocycles. 60: 1339. DOI: 10.3987/COM-03-9734 |
0.393 |
|
| 2003 |
Heindl C, Hübner H, Gmeiner P. Enantiospecific synthesis and receptor binding of novel dopamine receptor ligands employing natural 4-hydroxyproline as a practical and flexible building block Tetrahedron: Asymmetry. 14: 3153-3172. DOI: 10.1016/J.TETASY.2003.08.020 |
0.504 |
|
| 2003 |
Heindl C, Hübner H, Gmeiner P. Ex-chiral pool synthesis and receptor binding studies of 4-substituted prolinol derivatives Tetrahedron: Asymmetry. 14: 3141-3152. DOI: 10.1016/J.TETASY.2003.08.019 |
0.398 |
|
| 2003 |
Einsiedel J, Huebner H, Gmeiner P. Cyclic Amidines as Benzamide Bioisosteres: EPC Synthesis and SAR Studies Leading to the Selective Dopamine D4 Receptor Agonist FAUC 312. Cheminform. 34. DOI: 10.1002/CHIN.200330180 |
0.591 |
|
| 2002 |
Bettinetti L, Schlotter K, Hübner H, Gmeiner P. Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. Journal of Medicinal Chemistry. 45: 4594-7. PMID 12361386 DOI: 10.1021/JM025558R |
0.607 |
|
| 2002 |
Einsiedel J, Hübner H, Gmeiner P. Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). Bioorganic & Medicinal Chemistry Letters. 11: 2533-6. PMID 11549463 DOI: 10.1016/S0960-894X(01)00484-X |
0.573 |
|
| 2002 |
Löber S, Ortner B, Bettinetti L, Hübner H, Gmeiner P. Analogs of the dopamine D4 receptor ligand FAUC 113 with planar- and central-chirality Tetrahedron: Asymmetry. 13: 2303-2310. DOI: 10.1016/S0957-4166(02)00639-0 |
0.586 |
|
| 2001 |
Lehmann T, Hübner H, Gmeiner P. Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding Bioorganic &Amp; Medicinal Chemistry Letters. 11: 2863-2866. PMID 11597417 DOI: 10.1016/S0960-894X(01)00564-9 |
0.533 |
|
| 2001 |
Löber S, Hübner H, Utz W, Gmeiner P. 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). Journal of Medicinal Chemistry. 44: 2691-4. PMID 11495580 DOI: 10.1021/JM015522J |
0.593 |
|
| 2001 |
Lanig H, Utz W, Gmeiner P. 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. Journal of Medicinal Chemistry. 44: 1151-7. PMID 11312915 DOI: 10.1021/JM001055E |
0.49 |
|
| 2001 |
Ortner B, Waibel R, Gmeiner P. Indoloparacyclophanes: Synthesis and Dopamine Receptor Binding of a Novel Arylbioisostere This work was supported by the Fonds der Chemischen Industrie. Angewandte Chemie (International Ed. in English). 40: 1283-1285. PMID 11301452 DOI: 10.1002/1521-3773(20010401)40:7<1283::aid-anie1283>3.0.co;2-# |
0.422 |
|
| 2001 |
Einsiedel J, Thomas C, Hübner H, Gmeiner P. Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. Bioorganic & Medicinal Chemistry Letters. 10: 2041-4. PMID 10987445 DOI: 10.1016/S0960-894X(00)00405-4 |
0.543 |
|
| 2001 |
Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T. Synthesis and in vitro evaluation of iodine labelled pyrazolo[1,5-a]pyridines as highly selective dopamine D4 receptor ligands Journal of Labelled Compounds and Radiopharmaceuticals. 44: 849-858. DOI: 10.1002/JLCR.508 |
0.572 |
|
| 2001 |
Ortner B, Waibel R, Gmeiner P. Indoloparacyclophanes: Synthesis and Dopamine Receptor Binding of a Novel Arylbioisostere Angewandte Chemie. 113: 1323-1325. DOI: 10.1002/1521-3757(20010401)113:7<1323::AID-ANGE1323>3.0.CO;2-I |
0.489 |
|
| 2000 |
Hübner H, Kraxner J, Gmeiner P. Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. Journal of Medicinal Chemistry. 43: 4563-9. PMID 11087581 DOI: 10.1021/JM0009989 |
0.583 |
|
| 2000 |
Weber K, Ohnmacht U, Gmeiner P. Enantiopure 4- and 5-aminopiperidin-2-ones: regiocontrolled synthesis and conformational characterization as bioactive beta-turn mimetics. The Journal of Organic Chemistry. 65: 7406-16. PMID 11076597 DOI: 10.1021/JO000555C |
0.335 |
|
| 2000 |
Kraxner J, Hübner H, Gmeiner P. Azepino- and diazepinoindoles: synthesis and dopamine receptor binding profiles. Archiv Der Pharmazie. 333: 287-92. PMID 11039184 DOI: 10.1002/1521-4184(20009)333:9<287::AID-ARDP287>3.0.CO;2-R |
0.574 |
|
| 2000 |
Hübner H, Haubmann C, Utz W, Gmeiner P. Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype. Journal of Medicinal Chemistry. 43: 756-62. PMID 10691700 DOI: 10.1021/JM991098Z |
0.621 |
|
| 2000 |
Kraxner J, Huebner H, Gmeiner P. ChemInform Abstract: Azepino- and Diazepinoindoles: Synthesis and Dopamine Receptor Binding Profiles. Cheminform. 31: no-no. DOI: 10.1002/CHIN.200052143 |
0.479 |
|
| 2000 |
Einsiedel J, Thomas C, Huebner H, Gmeiner P. ChemInform Abstract: Phenyloxazoles and Phenylthiazoles as Benzamide Bioisosteres: Synthesis and Dopamine Receptor Binding Profiles. Cheminform. 31: no-no. DOI: 10.1002/CHIN.200047233 |
0.482 |
|
| 1999 |
Haubmann C, Hübner H, Gmeiner P. Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. Bioorganic & Medicinal Chemistry Letters. 9: 3143-6. PMID 10560741 DOI: 10.1016/S0960-894X(99)00540-5 |
0.571 |
|
| 1999 |
Haubmann C, Hübner H, Gmeiner P. 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. Bioorganic & Medicinal Chemistry Letters. 9: 1969-72. PMID 10450964 DOI: 10.1016/S0960-894X(99)00302-9 |
0.623 |
|
| 1999 |
Thomas C, Hübner H, Gmeiner P. Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid. Bioorganic & Medicinal Chemistry Letters. 9: 841-6. PMID 10206547 DOI: 10.1016/S0960-894X(99)00086-4 |
0.568 |
|
| 1999 |
Löber S, Hübner H, Gmeiner P. Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. Bioorganic & Medicinal Chemistry Letters. 9: 97-102. PMID 9990464 DOI: 10.1016/S0960-894X(98)00692-1 |
0.616 |
|
| 1999 |
Thomas C, Ohnmacht U, Niger M, Gmeiner P. Beta-analogs of PLG (L-prolyl-L-leucyl-glycinamide): ex-chiral pool syntheses and dopamine D2 receptor modulating effects. Bioorganic & Medicinal Chemistry Letters. 8: 2885-90. PMID 9873642 DOI: 10.1016/S0960-894X(98)00507-1 |
0.439 |
|
| 1996 |
Gmeiner P, Kärtner A, Mierau J. Synthesis and dopamine receptor binding studies of homochiral 8-aminopyrido[1,2-a]indoles. Archiv Der Pharmazie. 328: 626-8. PMID 7492270 DOI: 10.1002/ARDP.19953280712 |
0.568 |
|
| 1996 |
Gmeiner P, Bollinger B, Mierau J, Höfner G. Synthesis, pharmacological investigation and computational studies on a tricyclic ergoline analog with selective dopamine autoreceptor activity. Archiv Der Pharmazie. 328: 609-14. PMID 7492266 DOI: 10.1002/ARDP.19953280708 |
0.531 |
|
| 1996 |
Gmeiner P, Bollinger B, Lotter H. 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 Journal of Heterocyclic Chemistry. 33: 481-483. DOI: 10.1002/JHET.5570330243 |
0.465 |
|
| 1995 |
Gmeiner P, Sommer J, Höfner G. Synthesis and dopamine receptor binding of 3-phenylazepino[5,4,3-c,d]indole derivatives. Archiv Der Pharmazie. 328: 329-32. PMID 7611828 DOI: 10.1002/ARDP.19953280407 |
0.557 |
|
| 1993 |
Gmeiner P, Sommer J, Höfner G, Mierau J. Tricyclic azaergoline analogues: synthesis, structural modifications, and pharmacological studies. Archiv Der Pharmazie. 325: 649-55. PMID 1361322 DOI: 10.1002/ARDP.19923251007 |
0.486 |
|
| 1993 |
Gmeiner P, Sommer J, Mierau J, Höfner G. Dopamine autoreceptor agonists: computational studies, synthesis and biological investigations Bioorganic & Medicinal Chemistry Letters. 3: 1477-1483. DOI: 10.1016/S0960-894X(00)80003-7 |
0.339 |
|
| 1992 |
Gmeiner P, Mierau J, Höfner G. Enantiomerically pure aminoindolizines: bicyclic ergoline analogues with dopamine autoreceptor activity. Archiv Der Pharmazie. 325: 57-60. PMID 1605713 DOI: 10.1002/ARDP.19923250113 |
0.32 |
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