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JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).1 It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 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.2 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.3
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1. Pharmacology and antitussive efficacy of 4-
2. Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J. Neurosci. 25(12), 3126-3131 (2005).
3. Two TRPV1 receptor antagonists are effective in two different experimental models of migraine. J. Headache Pain 16, 57 (2015).