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A 784168 is a potent antagonist of TRPV1 receptor with pKi value of 7.15 [1].

The transient receptor potential cation channel subfamily V member 1 (TrpV1) receptor is a nonselective cation channel and distributes throughout the nervous system. TrpV1 receptor is activated by a wide variety of physical and chemical stimuli [1].

A 784168 is a potent TRPV1 receptor antagonist with pKi value of 7.15 for recombinant hTRPV1 receptor. In the Ca2+ flux assay, A 784168 inhibited 50 nM CAP-induced calcium flux with pIC50 value of 7.13 of the recombinant hTRPV1 receptor [1]. A 784168 inhibited TRPV1 activation by 50 nM capsaicin, pH 5.5, 3 μM NADA and 10 μM anandamide with IC50 values of 25, 14, 33.7, 35.1 nM, respectively. In rat dorsal root ganglion neurons, A 784168 inhibited 1 μM capsaicin-induced currents with IC50 value of 10 nM [2].

In CFA-induced thermal hyperalgesia, A-784168 (30 μM/kg) reduced capsaicin-induced nocifensive behaviors with ED50 value of 10 μM/kg [2]. In rats, A 784168 inhibited 1% formalin-induced secondary mechanical hyperalgesia and allodynia in the contralateral and ipsilateral paws [3].

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