|
|||||
|
|
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists |
|
| Authors: | Cowley Phillip M Baker James Buchanan Kirsteen I Carlyle Ian Clark John K Clarkson Thomas R Deehan Maureen Edwards Darren Kiyoi Yasuko Martin Iain Osbourn Dawn Walker Glenn Ward Nick Wishart Grant |
| Institution: | a Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK b Department of Molecular Pharmacology, MSD, Newhouse, Lanarkshire ML1 5SH, UK c Department of Pharmacology, MSD, Newhouse, Lanarkshire ML1 5SH, UK |
| Abstract: | The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB1 receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB1 antagonist with high predicted human oral bioavailability. |
| Keywords: | Cannabinoid CB1 Antagonist Indole Pharmacokinetics CYP3A4 Glucuronidation |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |