Biological Activity
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].
References
[1]. bianchi br, el kouhen r, neelands tr, et al. [3h]a-778317 [1-((r)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (trpv1) receptor. j pharmacol exp ther, 2007, 323(1): 285-293.
[2]. cui m, honore p, zhong c, et al. trpv1 receptors in the cns play a key role in broad-spectrum analgesia of trpv1 antagonists. j neurosci, 2006, 26(37): 9385-9393.
[3]. martínez-rojas va, barragán-iglesias p, rocha-gonzález hi, et al. role of trpv1 and asic3 in formalin-induced secondary allodynia and hyperalgesia. pharmacol rep, 2014, 66(6): 964-971.
