Chemical Name:3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyri
dine hydrochloride
Biological Activity:
Competitive P2X7 receptor antagonist
(pIC50 = 6.9 for the inhibition of Ca2+ influx in the
human recombinant P2X7 cell line). Devoid of activity at other P2
receptors (IC50 >> 10 μM). Possesses
antinociceptive activity in models of neuropathic pain in vivo.
Nelsonet
al (2006) Structure-activity relationship studies on a series of novel,
substituted 1-benzyl-5-phenyltetrazole P2X7 antagonist. J.Med.Chem. 49
3659. Donnelly-Roberts and Jarvis (2007) Discovery of P2X7
receptor-selective antagonists offers new insights into P2X7
receptor function and indicates a role in chronic pain states. Br.J.Pharmacol. 151
571. McGaraughtyet al (2007) P2X7-related modulation
of pathological nociception in rats. Neuroscience 146 1817.
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