1008529-54-1Relevant articles and documents
Discovery of TRPV1 antagonist ABT-116
Brown, Brian S.,Keddy, Ryan,Perner, Richard J.,DiDomenico, Stanley,Koenig, John R.,Jinkerson, Tammie K.,Hannick, Steven M.,McDonald, Heath A.,Bianchi, Bruce R.,Honore, Prisca,Puttfarcken, Pamela S.,Moreland, Robert B.,Marsh, Kennan C.,Faltynek, Connie R.,Lee, Chih-Hung
scheme or table, p. 3291 - 3294 (2010/08/07)
The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described. Biological studies demonstrated potent in vitro and in vivo activity for 21, as well as suitable physicochemical and pharmacokinetic pro