JNJ-17203212

JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel). It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Cay-92350, Cay-10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg. JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.Formal Name: 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide. CAS Number: 821768-06-3. Molecular Formula: C17H15F6N5O. Formula Weight: 419.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 249 nm. SMILES: FC(F)(F)C1=CC=C(NC(N2CCN(C3=NC=CC=C3C(F)(F)F)CC2)=O)N=C1. InChi Code: InChI=1S/C17H15F6N5O/c18-16(19,20)11-3-4-13(25-10-11)26-15(29)28-8-6-27(7-9-28)14-12(17(21,22)23)2-1-5-24-14/h1-5,10H,6-9H2,(H,25,26,29). InChi Key: JFRYYGVYCWYIDQ-UHFFFAOYSA-N.