824982-41-4 Usage
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 824982-41-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,2,4,9,8 and 2 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 824982-41:
(8*8)+(7*2)+(6*4)+(5*9)+(4*8)+(3*2)+(2*4)+(1*1)=194
194 % 10 = 4
So 824982-41-4 is a valid CAS Registry Number.
824982-41-4Relevant articles and documents
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists
Brown, Brian S.,Keddy, Ryan,Zheng, Guo Zhu,Schmidt, Robert G.,Koenig, John R.,McDonald, Heath A.,Bianchi, Bruce R.,Honore, Prisca,Jarvis, Michael F.,Surowy, Carol S.,Polakowski, James S.,Marsh, Kennan C.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 8516 - 8525 (2008/12/23)
A series of 1,2,3,6-tetrahydropyridyl-4-carboxamides, exemplified by 6, have been synthesized and evaluated for in vitro TRPV1 antagonist activity, and in vivo analgesic activity in animal pain models. The tetrahydropyridine 6 is a novel TRPV1 receptor an
Novel amides useful for treating pain
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Page/Page column 19, (2010/02/10)
The present invention relates to compounds of formula (I) that useful in treating pain.
Novel amides useful for treating pain
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Page/Page column 21, (2010/02/11)
The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.
