JNJ-17203212

• CAT Number: I004973
• CAS Number: 821768-06-3
• Molecular Formula: C17H15F6N5O
• Molecular Weight: 419.32
• Purity: ≥95%
• Target: TRP Channel
• Solubility: 10 mM in DMSO
• Storage: Store at +4C
• IC50: 65 nM (human TRPV1), 102 nM (rat TRPV1)

JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.IC50 value: 65 nM (human TRPV1), 102 nM (rat TRPV1)Target: TRPVin vivo: JNJ-17203212 reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. Throughout this study, 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] Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents core hypothermia evoked by sc capsaicin. Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents capsaicin-evoked hypothermia in a dose-response manner. [2]

Reference

1:Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64. doi: 10.1358/mf.2010.32.8.1507853. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats.Wiskur BJ,Tyler K,Campbell-Dittmeyer K,Chaplan SR,Wickenden AD,Greenwood-Van Meerveld B, PMID: 21132125 DOI: 10.1358/mf.2010.32.8.1507853 Abstract: This study examined the efficacy of a novel TRPV1 antagonist, JNJ-17203212, in two experimental rat models that exhibit a hypersensitive visceral motor response (VMR) to colorectal distension (CRD). In the first model, intraluminal administration of acetic acid (1% solution) into the distal colon produced an acute colonic hypersensitivity. In the second model, intraluminal administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS) into the distal colon produced a chronic, post-inflammatory colonic hypersensitivity 30 days post-TNBS administration. Throughout this study, 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. Intraluminal administration of acetic acid and TNBS resulted in increased VMR to CRD when compared to controls. In both groups, VMR to CRD was significantly reduced by administration of JNJ-17203212 at 30 mg/kg. The results of this study show that the selective TRPV1 antagonist, JNJ-17203212, reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. These data indicate that 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.Copyright 2010 Prous Science, S.A.U. or its licensors. All rights reserved.