| Identification | Back Directory | [Name]
A 784168 | [CAS]
824982-41-4 | [Synonyms]
A 784168
3'-(Trifluoromethyl)-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-
3'-(Trifluoromethyl)-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-c
3,6-Dihydro-3'-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2'-bipyridine]-4-carboxamide
[1(2H),2'-Bipyridine]-4-carboxamide, 3,6-dihydro-3'-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-
1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-3,6-dihydro-2H-pyridine-4-carboxamide | [Molecular Formula]
C19H15F6N3O3S | [MDL Number]
MFCD22373772 | [MOL File]
824982-41-4.mol | [Molecular Weight]
479.396 |
| Hazard Information | Back Directory | [Uses]
A 784168 is a known TRPV1 antagonist. | [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]. | [storage]
Store at RT | [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. |
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