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RP 67580Cat. No. 1635 |
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Chemical Name: (3aR,7aR)-Octahydro-2-[1-imino-2-(2-methoxyphenyl)ethyl]-7,7-diphenyl-4H-isoindol |
Biological Activity
Potent and selective tachykinin NK1 receptor antagonist (Ki values are 2.9 nM and > 10 μM for rat NK1, and rat NK2 and NK3 receptors respectively). Displays higher affinity at rat and mouse than human receptors. Antinociceptive in vivo, possibly partly via inhibition of calcium channels.Certificate of Analysis / Safety Data Sheet
References
Garret et al (1991) Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc.Natl.Acad.Sci.U.S.A. 88 10208. PMID: 1719549.
Fong et al (1992) Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580. J.Biol.Chem. 267 25668. PMID: 1281470.
Beaujouan et al (1993) Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br.J.Pharmacol. 108 793. PMID: 7682138.
Rupniak et al (1993) Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580. Br.J.Pharmacol. 110 1607. PMID: 8306108.
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Keywords: RP 67580, supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580
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