Catalog Number: 1635
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.
Background References
  1. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists.
    Beaujouan et al.
    Br.J.Pharmacol., 1993;108:793
  2. Pharmacological properties of a potent and selective nonpeptide substance P antagonist.
    Garret et al.
    Proc.Natl.Acad.Sci.U.S.A., 1991;88:10208
  3. Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580.
    Fong et al.
    J.Biol.Chem., 1992;267:25668
  4. Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580.
    Rupniak et al.
    Br.J.Pharmacol., 1993;110:1607
Citations:

The citations listed below are publications that use Tocris products. Selected citations for RP 67580 include:

4 Citations: Showing 1 - 4
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  1. Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine.
    Authors: Wang Et al.
    Am J Physiol Gastrointest Liver Physiol 2014;307:G719
  2. Activation of PAR(2) receptors sensitizes primary afferents and causes leukocyte rolling and adherence in the rat knee joint.
    Authors: Russell Et al.
    Br J Pharmacol 2012;167:1665
  3. Protease-activated receptor 2-mediated protection of myocardial ischemia-reperfusion injury: role of transient receptor potential vanilloid receptors.
    Authors: Zhong and Wang
    Am J Physiol Regul Integr Comp Physiol 2009;297:R1681
  4. TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats.
    Authors: Wang Et al.
    J Neurosci 2008;294:R1517

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