Description
JNJ-17203212 is a novel, reversible, and selective TRPV1 antagonist which could not inhibit related TRP channels. Its IC50 values are 65 nM and 102 nM for human TRPV1 and rat TRPV1. It could reduce sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. It inhibits capsaicin- and H+-induced channel activation, which pIC50 values are 6.32 and 7.23 respectively. It exhibits antitussive and analgesic activity in vivo