A 784168 - CAS 824982-41-4
Category: Inhibitor
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TRP Channel
A 784168 is a potent and selective TRPV1 antagonist (IC50 = 25 nM for inhibition of TRPV1 activation by 50 nM capsaicin) exhibiting no activity against a range of receptors such as TRPA1, GABA, opioid, and purinergic receptors.
Brife Description:
TRPV1 antagonist
≥99% by HPLC
3,6-Dihydro-3'-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2'-bipyridine]-4-carboxamide; 1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-3,6-dihydro-2H-pyridine-4-carboxamide
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1.TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists.
Cui M;Honore P;Zhong C;Gauvin D;Mikusa J;Hernandez G;Chandran P;Gomtsyan A;Brown B;Bayburt EK;Marsh K;Bianchi B;McDonald H;Niforatos W;Neelands TR;Moreland RB;Decker MW;Lee CH;Sullivan JP;Faltynek CR J Neurosci. 2006 Sep 13;26(37):9385-93.
Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. In addition to expression in primary afferents, TRPV1 is also expressed in the CNS. To test the hypothesis that the CNS plays a differential role in the effect of TRPV1 antagonists in various types of pain, the analgesic effects of two TRPV1 antagonists with similar in vitro potency but different CNS penetration were compared in vivo. Oral administration of either A-784168 (1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-1,2,3,6-tetrahydropyridine-4-carboxamide) (good CNS penetration) or A-795614 (N-1H-indazol-4-yl-N'-[(1R)-5-piperidin-1-yl-2,3-dihydro-1H-inden-1-yl]urea) (poor CNS penetration) blocked capsaicin-induced acute pain with the same potency. In complete Freund's adjuvant (CFA)-induced chronic inflammatory pain, oral administration of either compound blocked thermal hyperalgesia with similar potency. Furthermore, intraplantar or intrathecal administration of A-784168 blocked CFA-induced thermal hyperalgesia, suggesting that both peripheral and CNS TRPV1 receptors may play a role in inflammatory thermal hyperalgesia.
2.Role of TRPV1 and ASIC3 in formalin-induced secondary allodynia and hyperalgesia.
Martínez-Rojas VA;Barragán-Iglesias P;Rocha-González HI;Murbartián J;Granados-Soto V Pharmacol Rep. 2014 Dec;66(6):964-71. doi: 10.1016/j.pharep.2014.06.011. Epub 2014 Jun 24.
BACKGROUND: ;In the present study we determined the role of transient receptor potential V1 channel (TRPV1) and acid-sensing ion channel 3 (ASIC3) in chronic nociception.;METHODS: ;1% formalin was used to produce long-lasting secondary allodynia and hyperalgesia in rats. Western blot was used to determine TRPV1 and ASIC3 expression in dorsal root ganglia.;RESULTS: ;Peripheral ipsilateral, but not contralateral, pre-treatment (-10min) with the TRPV1 receptor antagonists capsazepine (0.03-0.3μM/paw) and A-784168 (0.01-1μM/paw) prevented 1% formalin-induced secondary mechanical allodynia and hyperalgesia in the ipsilateral and contralateral paws. Likewise, peripheral ipsilateral, but not contralateral, pre-treatment with the non-selective and selective ASIC3 blocker benzamil (0.1-10μM/paw) and APETx2 (0.02-2μM/paw), respectively, prevented 1% formalin-induced secondary mechanical allodynia and hyperalgesia in both paws. Peripheral ipsilateral post-treatment (day 6 after formalin injection) with capsazepine (0.03-0.3μM/paw) and A-784168 (0.01-1μM/paw) reversed 1% formalin-induced secondary mechanical allodynia and hyperalgesia in both paws. In addition, peripheral ipsilateral post-treatment with benzamil (0.
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CAS 824982-41-4 A 784168

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