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Potent and selective NK1 receptor antagonist. Potently inhibits substance P binding to NK1 receptors (pKi = 10.1 to 10.5). Displays antiemetic activity in vivo.
Sold for research purposes under agreement from GlaxoSmithKline
|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 437.37. 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|
|0.2 mM||11.43 mL||57.16 mL||114.32 mL|
|1 mM||2.29 mL||11.43 mL||22.86 mL|
|2 mM||1.14 mL||5.72 mL||11.43 mL|
|10 mM||0.23 mL||1.14 mL||2.29 mL|
References are publications that support the biological activity of the product.
Beattie et al (1995) The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist. Br.J.Pharmacol. 116 3149 PMID: 8719789
Gardner et al (1995) The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040. Br.J.Pharmacol. 116 3158 PMID: 8719790
Ward et al (1995) Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. J.Med.Chem. 38 4985 PMID: 8544174
If you know of a relevant reference for GR 203040, please let us know.
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Keywords: GR 203040, GR 203040 supplier, GR203040, potent, selective, tachykinin, NK1, receptor, antagonists, antagonism, antiemetics, Receptor, 4647, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.