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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.
Nelson et al (2006) Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. 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. McGaraughty et al (2007) P2X7-related modulation of pathological nociception in rats. Neuroscience 146 1817.
See how others have used A 438079 hydrochloride. Click on the entry to view the PubMed entry .
PMID: # 26739809 2016. Sci Rep. 6: 19108.
PMID: # 22986947 2013. Toxicol. Sci. 131: 325-35.
PMID: # 22865777 Ito, G. et al. 2013. Eur J Pain. 17: 185-199.
PMID: # 22343416 Chatterjee, S. et al. 2012. Free Radic. Biol. Med. 52: 1666-79.
PMID: # 21763420 Ohshima, Y. et al. 2011. Free Radic. Biol. Med. 51: 1240-1248.
PMID: # 19171786 Díaz-Hernández, M. et al. 2009. FASEB J. 23: 1893-1906.
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