Description
A TRPV1 antagonist (Ki = 72 nM for the recombinant guinea pig channel); inhibits capsaicin- or pH decrease-induced guinea pig TRPV1 channel activation (IC50s = 58 and 470 nM, respectively); reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs at 20 mg/kg; reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain at 30 mg/kg; decreases capsaicin-induced production of CGRP and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine