Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Stephen A. Espitia"'
Autor:
Hussien A. Al-Shamma, Michael M. Morgan, William Thomsen, Dominic P. Behan, Derek T. Chalmers, Stephen A. Espitia, Diane Yuskin, Weichao Chen, Michael Gary Martin, Andrew J. Grottick, Brian R. Smith, Hazel Reyes-Saldana, Kevin Whelan, Frédérique Menzaghi
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 325:577-587
5-Hydroxytryptamine (5-HT)(2C) receptor agonists hold promise for the treatment of obesity. In this study, we describe the in vitro and in vivo characteristics of lorcaserin [(1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3 benzazepine], a selective, h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bbef1a6f7731c7ae52a0600fc2b937d
https://doi.org/10.1124/jpet.107.133348
https://doi.org/10.1124/jpet.107.133348
Autor:
Edward R. Whittemore, Minhtam Tran, David Rock, Richard M. Woodward, Zhang-Lin Zhou, Sui Xiong Cai, Christopher S. Konkoy, Stephen A. Espitia, Lawrence D. Wise, Christopher F. Bigge, John F. W. Keana, Jon E. Hawkinson, Eckard Weber, Peter A. Boxer, Linda L. Coughenour
Publikováno v:
Journal of Medicinal Chemistry. 42:2993-3000
A structure-based search and screen of our compound library identified N-(2-phenoxyethyl)-4-benzylpiperidine (8) as a novel N-methyl-D-aspartate (NMDA) receptor antagonist that has high selectivity for the NR1/2B subunit combination (IC(50) = 0.63 mi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43f0076ffe71bb601601d1cf2ac46fcd
https://doi.org/10.1021/jm990246i
https://doi.org/10.1021/jm990246i
Autor:
Eckard Weber, Minhtam Tran, Sui Xiong Cai, Jin-Cheng Huang, Victor I. Ilyin, Richard M. Woodward, John F. W. Keana, Stephen A. Espitia, Jon E. Hawkinson
Publikováno v:
Journal of Medicinal Chemistry. 40:3679-3686
A group of 5-aza-7-substituted-1,4-dihydroquinoxaline-2,3-diones (QXs) and the corresponding 5-(N-oxyaza)-7-substituted QXs were prepared and evaluated as antagonists of ionotropic glutamate receptors. The in vitro potency of these QXs was determined
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df962021acf5438841b9472334bb7ab6
https://doi.org/10.1021/jm970396y
https://doi.org/10.1021/jm970396y
Autor:
Jon E. Hawkinson, Stephen A. Espitia
Publikováno v:
European Journal of Pharmacology. 329:213-221
AMPA receptors can be labeled using the agonist radioligands [3H](R,S)-α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ([3H](R,S)-AMPA), [3H](S)-AMPA or [3H](S)-5-fluorowillardiine. In the presence of KSCN, [3H](R,S)-AMPA and [3H](S)-AMPA bind
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5557be3881d6dbbd625dce3dbf795a67
https://doi.org/10.1016/s0014-2999(97)89182-0
https://doi.org/10.1016/s0014-2999(97)89182-0
Autor:
Minhtam Tran, Stephen A. Espitia, John F. W. Keana, Richard M. Woodward, Sunil M. Kher, Zhang-Lin Zhou, Victor I. Ilyin, Jon E. Hawkinson, Eckard Weber, Sui Xiong Cai
Publikováno v:
Journal of Medicinal Chemistry. 40:730-738
We report on a series of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones (QXs), prepared as a continuation of our structure-activity relationship (SAR) study of QXs as antagonists for the glycine site of the N-methyl-D-aspartate (NMDA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51ed936d6d6a797f5ec54af8674020c0
https://doi.org/10.1021/jm960654b
https://doi.org/10.1021/jm960654b
Autor:
Rita R. Chen, Stephen A. Espitia, Emily B. Prieto, James Tsai, Douglas M. Park, Michael Morgan, Albert S. Ren, Scott A. Estrada, Jon A. Covel, Dipanjan Sengupta, Charlemagne S. Gallardo, Brian M. Smith, Peter I. Dosa, M. J. Martin, Kevin Whelan, Christina Bjenning, Nigel Robert Arnold Beeley, Jeffrey Smith, Jeffrey A. Schultz, Charles A Gilson, William Thomsen, Robert R. Webb, Hazel R. Saldana, Frederique Menzaghi, Andrew J. Grottick
Publikováno v:
Journal of medicinal chemistry. 51(2)
The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::023ac9ea3dfbee3121f4be18befd7671
https://pubmed.ncbi.nlm.nih.gov/18095642
https://pubmed.ncbi.nlm.nih.gov/18095642
Autor:
Jon L. Wright, Tracy F. Gregory, Suzanne R. Kesten, Peter A. Boxer, Kevin A. Serpa, Leonard T. Meltzer, Lawrence D. Wise, Stephen A. Espitia, Christopher S. Konkoy, Edward R. Whittemore, Richard M. Woodward
Publikováno v:
Journal of medicinal chemistry. 43(18)
4-[4-(4-Benzylpiperidin-1-yl)but-1-ynyl]phenol (8) and 4-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]phenol (9) are potent NR1A/2B receptor antagonists (IC(50) values 0.17 and 0.10 microM, respectively). Administered intraperitoneally, they both potentiat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0ce78d2d0d1f7b641bd2e7194787fe2
https://pubmed.ncbi.nlm.nih.gov/10978188
https://pubmed.ncbi.nlm.nih.gov/10978188
Publikováno v:
European journal of pharmacology. 389(2-3)
Nociceptin (orphanin FQ) is the recently discovered peptide agonist for the orphan receptor opioid receptor-like 1 (ORL1). Despite the high sequence homology between ORL1 and the opioid receptors, most opioids lack affinity for the nociceptin recepto
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe3b498a1c1c318ff2178e741198248f
https://pubmed.ncbi.nlm.nih.gov/10688973
https://pubmed.ncbi.nlm.nih.gov/10688973
Autor:
John F. W. Keana, Richard M. Woodward, Eckard Weber, Anthony P. Guzikowski, Daniel F. Nogales, Stephen A. Espitia, Jon E. Hawkinson, James E. Huettner, Minhtam Tran, Sui Xiong Cai
Publikováno v:
Journal of medicinal chemistry. 39(23)
A series of aromatic and azepine ring-modified analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione (HBAD) were synthesized and evaluated as antagonists at NMDA receptor glycine sites. Aromatic ring-modified HBADs were generally prepared via a Schmidt rea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ee176df0ba6d7e18a19ae74e5ec0f1a
https://pubmed.ncbi.nlm.nih.gov/8917653
https://pubmed.ncbi.nlm.nih.gov/8917653
Autor:
Stephen A. Espitia, Eckard Weber, John F. W. Keana, Jon E. Hawkinson, Richard M. Woodward, Victor I. Ilyin, Hua Zheng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:439-440
A series of 1-hydroxy-1,4-dihydroquinoxaline-2,3-diones was synthesized and assayed for NMDA receptor glycine site antagonism. Except for 4a, these were found to be 3–80 times weaker antagonists than the analogous 1,4-dihydroquinoxaline-2,3-diones.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::11d9879a1d967ace8bf1b6608cea21f2
https://doi.org/10.1016/0960-894x(96)00036-4
https://doi.org/10.1016/0960-894x(96)00036-4