JNJ-17203212

TRPV1拮抗剂（重组豚鼠通道的Ki=72nM）；抑制辣椒素或pH降低引起的豚鼠TRPV1通道激活（IC50s分别为58和470nM）；20mg/kg剂量下减少豚鼠因柠檬酸或辣椒素引起的咳嗽次数；30mg/kg剂量下减少骨癌痛小鼠模型中自发性和心悸引起的畏缩和警觉；降低偏头痛大鼠模型中辣椒素诱导的CGRP产生和炎性汤诱导的三叉神经cfos表达。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.分子式C17H15F6N5O分子量419.3FC(F)(F)C1=CC=C(NC(N2CCN(C3=NC=CC=C3C(F)(F)F)CC2)=O)N=C1