JNJ-39729209 is a potent, selective TRPV1 antagonist with binding pKi of 7.8 and 7.9 for human and rat TRPV1, respectively.
JNJ-39729209 inhibits proton activation of human and rat TRPV1 receptors with pIC50s of 7.9 and 8.5, respectively, also prevents TRPV1 activation by capsaicin and heat.
JNJ-39729209 shows no agonist or antagonist activity forTRPV2, hTRPV4, or hTRPA1 at 10 uM.
JNJ-39729209 blocks capsaicin-induced hypotension, inducesa mild hyperthermia and inhibits capsaicin-induced hypothermia in vivo.
JNJ-39729209shows significant efficacy against carrageenan- and CFA-evoked thermal hyperalgesia and exhibits significant anti-tussive activity in a guinea-pig model of capsaicin-induced cough.
