| Literature DB >> 16806913 |
Susan M Westaway1, Ying-Kit Chung, John B Davis, Vicky Holland, Jeffrey C Jerman, Stephen J Medhurst, Harshad K Rami, Geoffrey Stemp, Alexander J Stevens, Mervyn Thompson, Kim Y Winborn, James Wright.
Abstract
Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent potency at human, guinea pig and rat TRPV1, a favourable in vitro DMPK profile and activity in an in vivo model of inflammatory pain.Entities:
Mesh：
Substances：
Year: 2006 PMID： 16806913 DOI： 10.1016/j.bmcl.2006.06.026
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823