JNJ-17203212 是一种竞争性TRPV1选择性拮抗剂。它被开发用于疼痛处理的研究。

JNJ-17203212 is a potent and selective antagonist of TRPV1 (human TRPV1 and rat TRPV1, IC50 of 65 nM and 102 nM).

TRPV1 antagonist, JNJ-17203212, reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity.??TRPV1 is involved in the pathogenesis of visceral hypersensitivity and that JNJ-17203212 may be a potential therapeutic agent for functional bowel disorders characterized by abdominal hypersensitivity, such as irritable bowel syndrome[1].

Colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle[1].

821768-06-3

C17H15F6N5O

419.32

DMSO:100 mg/mL (238.48 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years