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Category:
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7TM Receptors Peptides (Neuropeptides)Tachykinin ReceptorsNK-1 Receptor
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Cat.No.
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Product Name
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1635 |
RP 67580
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Price and Availability
Click here for full price details of
RP 67580
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Chemical Name:
(3aR,7aR)-Octahydro-2-[1-imino-2-(2-methoxyphenyl)ethyl
]-7,7-diphenyl-4H-isoindol |
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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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Garret et
al (1991) Pharmacological properties of a potent and selective nonpeptide
substance P antagonist. Proc.Natl.Acad.Sci.USA 88 10208. 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. 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. Rupniak et al (1993)
Antinociceptive activity of NK1 receptor antagonists: non-specific
effects of racemic RP67580. Br.J.Pharmacol. 110 1607.
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Keywords: RP 67580, Peptides (Neuropeptides), Potent & Selective NK1 Antagonist, RP67580, Tocris Bioscience
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