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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 438.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.28 mL||11.4 mL||22.8 mL|
|5 mM||0.46 mL||2.28 mL||4.56 mL|
|10 mM||0.23 mL||1.14 mL||2.28 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
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
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
Rupniak et al (1993) Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580. Br.J.Pharmacol. 110 1607 PMID: 8306108
If you know of a relevant reference for RP 67580, please let us know.
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Keywords: RP 67580, RP 67580 supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, Receptor, 1635, Tocris Bioscience
4 Citations for RP 67580
Citations are publications that use Tocris products. Selected citations for RP 67580 include:
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
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
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.