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A 803467Cat. No. 2976 |
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Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide |
Biological Activity
Selective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively). Shows no significant activity against TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.Certificate of Analysis / Safety Data Sheet
References
Jarvis et al (2007) A-803467, a potent and selective NaV1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc.Natl.Acad.Sci. 104 8520.
Rush and Cummins (2007) Painful research: identification of a small-molecule inhibitor that selectively targets NaV1.8 sodium channels. Mol.Interv. 7 192. PMID: 17827438.
Kort et al (2008) Discovery and biological evaluation of 5-Aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. J.Med.Chem. 51 407. PMID: 18176998.
McGaraughty et al (2008) A selective NaV1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J.Pharmacol.Exp.Ther. 324 1204. PMID: 18089840.
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Keywords: A 803467, supplier, Selective, NaV18, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, A803467
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