Zobrazeno 1 - 10
of 98
pro vyhledávání: '"Graeme Semple"'
Autor:
Thuy-Anh Tran, Bryan Kramer, Young-Jun Shin, Quyen-Quyen Do, Brett Ullman, Vasudeva Sagi, John W. Adams, Yunqing Shi, Hsin-Hui Shu, David J. Unett, Joel Gatlin, Michael E. Morgan, Jaimie Reuter, Anthony Blackburn, Carleton R. Sage, Graeme Semple
Publikováno v:
Results in Chemistry, Vol 4, Iss , Pp 100518- (2022)
The design of a new series of β3-Adrenergic receptor (β3-AdrR) antagonists is described. The use of a spiro building block in the core of the molecule provided novel compounds with reduced aromaticity and antagonist activity at the human β3-AdrR.
Externí odkaz:
https://doaj.org/article/6533cc49f4b54ba9916eb28cfabb9af8
Autor:
Alan Wise, M. Gerard Waters, Graeme Semple, Stefan Offermanns, Timothy W. Lovenberg, Adriaan P. IJzerman, Steven L. Colletti
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2023
The hydroxycarboxylic acid family of receptors (ENSFM00500000271913, nomenclature as agreed by the NC-IUPHAR Subcommittee on Hydroxycarboxylic acid receptors [36, 12]) respond to organic acids, including the endogenous hydroxy carboxylic acids 3-hydr
Autor:
Thomas O, Schrader, Xiuwen, Zhu, Michelle, Kasem, Albert, Ren, Chunyan, Liu, Chunrui, Wu, Huong, Dang, Minh, Le, Joel, Gatlin, Kelli, Chase, John, Frazer, Kevin T, Whelan, Andrew J, Grottick, Clayton, Hutton, Jeremy, Barden, Chuan, Chen, Alvaro, Ortiz, Konrad, Feichtinger, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 38
A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT
Autor:
Xiaohua Chen, Ibragim Gaidarov, John W. Adams, John Frazer, Graeme Semple, Todd Anthony, Joel Gatlin, David J. Unett
Publikováno v:
Cellular Signalling. 50:9-24
Angiotensin (1-7) has been reported to be a ligand for the GPCR MAS1. Small molecule MAS1 modulators have also been recently characterized. Aside from convincing evidence for MAS1 activation of Gq signaling, little is known about MAS1 mediated signal
Autor:
Albert, Ren, Xiuwen, Zhu, Konrad, Feichtinger, Juerg, Lehman, Michelle, Kasem, Thomas O, Schrader, Amy, Wong, Huong, Dang, Minh, Le, John, Frazer, David J, Unett, Andrew J, Grottick, Kevin T, Whelan, Michael E, Morgan, Carleton R, Sage, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(5)
A series of potential new 5-HT
Autor:
Michelle Kasem, Graeme Semple, Sufang Li, Chunyan Liu, Albert S. Ren, Xiuwen Zhu, Thomas O. Schrader, Chunrui Wu
Publikováno v:
Tetrahedron Letters. 59:2030-2033
Asymmetric syntheses of N-protected (R)-4-halo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines, advanced intermediates for the synthesis of highly potent and selective 5-HT2C agonists, are described. The key transformation involves ring
Autor:
Sangdon Han, David J. Unett, Michelle Solomon, Ibragim Gaidarov, Joel Gatlin, Xiaohua Chen, Graeme Semple, Todd Anthony, David Mills
Publikováno v:
Pharmacological Research. 131:185-198
GPR84 is an orphan G-protein coupled receptor, expressed on monocytes, macrophages and neutrophils and is significantly upregulated by inflammatory stimuli. The physiological role of GPR84 remains largely unknown. Medium chain fatty acids (MCFA) acti
Autor:
Michelle Solomon, Lars Thoresen, Robert M. Jones, Andrew J. Grottick, David J. Unett, Abu J.M. Sadeque, Chuan Chen, Ibragim Gaidarov, Hussien A. Al-Shamma, Jayant Thatte, Graeme Semple, Jae-Kyu Jung, Amin Usmani, Jeremy Barden, Xiuwen Zhu, Woo Hyun Yoon, Sangdon Han, Christopher Ronald J
Publikováno v:
ACS Medicinal Chemistry Letters. 8:1309-1313
The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in
Autor:
Minh Le, Albert S. Ren, Andrew J. Grottick, Graeme Semple, Kevin Whelan, Kelli Chase, Carleton R. Sage, Bilal Al Doori, Jenny Dong, Michelle Kasem, Chunrui Wu, Konrad Feichtinger, Jing Wei, Thomas O. Schrader, Huong T. Dang, Joel Gatlin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5877-5882
The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C receptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for bot
Autor:
Clayton Hutton, Andrew J. Grottick, Graeme Semple, Konrad Feichtinger, Thomas O. Schrader, Jeremy Barden, Chunyan Liu, Kevin Whelan, Xiuwen Zhu, Chuan Chen, Chunrui Wu, John Frazer, Huong T. Dang, Joel Gatlin, Alvaro Ortiz, Minh Le, Albert S. Ren, Michelle Kasem, Kelli Chase
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 38:127872
A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT2C receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based