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pro vyhledávání: '"Selective receptor modulator"'
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Autor:
Michael J. Stocks, Iain Walters, Steve Thom, Kenneth McKechnie, John Dixon, Nicholas Kindon, Premji Meghani, Iain G. Dougall, Timothy Johnson, Andrew M. Davis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4849-4853
The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f26f0469d7b8d29311af21124208ddba
https://doi.org/10.1016/j.bmcl.2017.09.043
https://doi.org/10.1016/j.bmcl.2017.09.043
Autor:
Yan-Ran Wu, Jie Tang, Jian-Zhong Chen, Jing Li, Yan-Hui Duan, Fan Yang, Ji Yueyang, Xin Xie, Shi Ying, Xiao-Yu Xie, Zhi-Long Wang, Hendra Gunosewoyo, Li-Fang Yu
Publikováno v:
Journal of Medicinal Chemistry. 60:7067-7083
Selective CB2 agonists represent an attractive therapeutic strategy for the treatment of a variety of diseases without psychiatric side effects mediated by the CB1 receptor. We carried out a rational optimization of a black market designer drug SDB-0
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bd888904ea93247a255963a15bf3575
https://doi.org/10.1021/acs.jmedchem.7b00724
https://doi.org/10.1021/acs.jmedchem.7b00724
Autor:
Bryan L. Roth, Alan P. Kozikowski, Terry P. Kenakin, Hu Zhu, John D. McCorvy, Jianjun Cheng, Patrick M. Giguere
Publikováno v:
Journal of Medicinal Chemistry. 59:9866-9880
On the basis of the structural similarity of our previous 5-HT2C agonists with the melatonin receptor agonist tasimelteon and the putative biological cross-talk between serotonergic and melatonergic systems, a series of new (2,3-dihydro)benzofuran-ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0a3eae7de4067f01b8bba8d7608f8a4b
https://doi.org/10.1021/acs.jmedchem.6b01194
https://doi.org/10.1021/acs.jmedchem.6b01194
Autor:
Philip R. Kym, Arthur Gomtsyan, Gregory A. Gfesser, Bin Li, Regina M. Reilly, Bruce Clapham, Jerome F. Daanen, Rodger F. Henry, Torben R. Neelands, Pamela S. Puttfarcken, Susan M. Huang, Robert G. Schmidt, Robert J. Altenbach, S.K. Joshi, Huaqing Liu, Marlon D. Cowart, David N. Whittern, Phil B. Cox, Jill-Desiree Brederson, Michael J. Dart, Anurupa Shrestha, Donna Gauvin, Michael E. Kort, Erol K. Bayburt, Ping Song, Steve McGaraughty, Connie R. Faltynek, Heath A. McDonald, Patricia N. Banfor, Diana Schmidt, Eric A. Voight, Mohamad Shebley, Jason A. Segreti
Publikováno v:
Journal of Medicinal Chemistry. 59:4926-4947
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd1b773984159dd5e2a719a0398228e6
https://doi.org/10.1021/acs.jmedchem.6b00287
https://doi.org/10.1021/acs.jmedchem.6b00287
Autor:
Catia Lambertucci, Diego Dal Ben, Michela Buccioni, Rosaria Volpini, Gabriella Marucci, Ajiroghene Thomas
Publikováno v:
Scopus-Elsevier
In this work, we have highlighted data reported in the literature trying to draw a complete picture of the structures and biological activity of agonists and orthosteric antagonists of P2X receptors. Actually, only few P2X receptor agonists have been
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acf4447b79e261053cba8de40532d16f
https://doi.org/10.2174/0929867321666141215093513
https://doi.org/10.2174/0929867321666141215093513
Autor:
Mange Ram Yadav, Prashant R. Murumkar, Mahesh A. Barmade, Mahesh Shidore, Jigar Thanki, Jatin Machhi
Publikováno v:
RSC Advances. 5:91908-91921
In search of potent and selective 5-HT2C receptor agonists, a series of novel 3-substituted 1-methyl-3-benzazepin-2-ones and 8-chloro-1-methyl-3-benzazepin-2-ones have been synthesized and evaluated for their 5-HT2C receptor agonistic potential. 5-HT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7f15c8e684361f7c85a92c0df5ad004f
https://doi.org/10.1039/c5ra17718a
https://doi.org/10.1039/c5ra17718a
Autor:
Teija Parkkari, Ettore Novellino, Clementina Manera, Luciana Marinelli, Giuseppe Saccomanni, Simone Saguto, Marco Allarà, Marco Macchia, Agostino Bruno, Alessia Ligresti, Chiara Arena, Simone Bertini, Juha R. Savinainen, Vincenzo Di Marzo
Publikováno v:
European journal of medicinal chemistry 90 (2014): 526–536. doi:10.1016/j.ejmech.2014.11.066
info:cnr-pdr/source/autori:Bertini S.; Parkkari T.; Savinainen J.R.; Arena C.; Saccomanni G.; Saguto S.; Ligresti A.; Allara M.; Bruno A.; Marinelli L.; Di Marzo V.; Novellino E.; Manera C.; Macchia M./titolo:Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands/doi:10.1016%2Fj.ejmech.2014.11.066/rivista:European journal of medicinal chemistry/anno:2014/pagina_da:526/pagina_a:536/intervallo_pagine:526–536/volume:90
info:cnr-pdr/source/autori:Bertini S.; Parkkari T.; Savinainen J.R.; Arena C.; Saccomanni G.; Saguto S.; Ligresti A.; Allara M.; Bruno A.; Marinelli L.; Di Marzo V.; Novellino E.; Manera C.; Macchia M./titolo:Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands/doi:10.1016%2Fj.ejmech.2014.11.066/rivista:European journal of medicinal chemistry/anno:2014/pagina_da:526/pagina_a:536/intervallo_pagine:526–536/volume:90
The CB2 receptor is a therapeutic target of increasing importance for several diseases, including pain, inflammation, neurodegeneration, cancer and osteoporosis. While several compounds showing CB2-selective agonist or inverse agonist properties have
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af40304bd7a3fe76c334f68b8dea7871
https://doi.org/10.1016/j.ejmech.2014.11.066
https://doi.org/10.1016/j.ejmech.2014.11.066
Autor:
Natsumi Yuzawa, Koji Kawai, Yuji Sugawara, Shinya Suzuki, Riichiro Tsuji, Chihiro Kaneko, Ryuji Tanimura, Mai Yagi
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(16)
κ-Opioid receptor agonists with high selectivity over the μ-opioid receptor are attractive targets in the development of drugs for pain and pruritus. We previously reported the synthesis of 10α-hydroxy TRK-820 (1). In this study, we elucidated the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c6acad81e3ab0a6a8c50f5fcdd06a18
https://pubmed.ncbi.nlm.nih.gov/30579796
https://pubmed.ncbi.nlm.nih.gov/30579796
Publikováno v:
Steroids. 90:30-38
Our understanding of the molecular mechanisms underlying the pharmacological actions of estrogen receptor (ER) ligands has evolved considerably in recent years. Much of this knowledge has come from a detailed dissection of the mechanism(s) of action
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59612a2be95a0f48b373e9f703b1853e
https://doi.org/10.1016/j.steroids.2014.07.013
https://doi.org/10.1016/j.steroids.2014.07.013