1. Discovery of TRPV1 antagonist ABT-116
- Author
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Tammie K. Jinkerson, Brian S. Brown, Bruce R. Bianchi, Richard J. Perner, Heath A. McDonald, Ryan G. Keddy, Stanley Didomenico, Connie R. Faltynek, Pamela S. Puttfarcken, Prisca Honore, Kennan C. Marsh, Steven M. Hannick, Robert B. Moreland, John R. Koenig, and Chih-Hung Lee
- Subjects
Indazoles ,Clinical Biochemistry ,Analgesic ,TRPV1 ,Pharmaceutical Science ,TRPV Cation Channels ,Pharmacology ,Biochemistry ,chemistry.chemical_compound ,Structure-Activity Relationship ,Pharmacokinetics ,In vivo ,Drug Discovery ,Structure–activity relationship ,Animals ,Humans ,Molecular Biology ,Indazole ,Analgesics ,Chemistry ,Phenylurea Compounds ,Organic Chemistry ,Antagonist ,In vitro ,Rats ,Molecular Medicine - Abstract
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 properties for advancement to clinical development for pain management.
- Published
- 2010