RP 67580

Cat. No. 1635

RP 67580 C29H30N2O2 [135911-02-3]

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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.

Technical Data

M.Wt:
438.57
Formula:
C29H30N2O2
Solubility:
Soluble to 100 mM in ethanol and to 50 mM in DMSO
Purity:
>97 %
Storage:
Store at -20°C
CAS No:
135911-02-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for RP 67580 include:

Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719. PMID: 25147231.

Russell et al (2012) Activation of PAR(2) receptors sensitizes primary afferents and causes leukocyte rolling and adherence in the rat knee joint. Br J Pharmacol 167 1665. PMID: 22849826.

Zhong and Wang (2009) Protease-activated receptor 2-mediated protection of myocardial ischemia-reperfusion injury: role of transient receptor potential vanilloid receptors. Am J Physiol Regul Integr Comp Physiol 297 R1681. PMID: 19812353.

Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. J Neurosci 294 R1517. PMID: 18337316.

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Keywords: RP 67580, supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, Tocris Bioscience, NK1 Receptor Antagonist products

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