A-425619

A TRPV1 antagonist, selective for TRPV1 over a panel of 83 receptors, enzymes, transporters, and ion channels at 10 µM, inhibits capsaicin-, NADA-, anandamide-, or acid-induced increases in intracellular calcium in HEK293 cells expressing human TRPV1 (IC50s = 5, 4, 3, and 2 nM, respectively), increases core body temperature in rats at 30 mg/kg, increases the paw withdrawal threshold in several rodent models of inflammatory, neuropathic, osteoarthritic, and postoperative pain. Formulation: A solid. InChI: InChI=1S/C18H14F3N3O/c19-18(20,21)14-6-4-12(5-7-14)10-23-17(25)24-16-3-1-2-13-11-22-9-8-15(13)16/h1-9,11H,10H2,(H2,23,24,25). InChIKey: SJGVXVZUSQLLJB-UHFFFAOYSA-N. SMILES: O=C(NCC1=CC=C(C(F)(F)F)C=C1)NC2=CC=CC3=C2C=CN=C3