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A potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. Inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.
Sold with the permission of GlaxoSmithKline
|Storage||Desiccate 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 414.54. 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|
|0.5 mM||4.82 mL||24.12 mL||48.25 mL|
|2.5 mM||0.96 mL||4.82 mL||9.65 mL|
|5 mM||0.48 mL||2.41 mL||4.82 mL|
|25 mM||0.1 mL||0.48 mL||0.96 mL|
References are publications that support the biological activity of the product.
Beresford et al (1995) GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur.J.Pharmacol. 272 241 PMID: 7713168
Walsh et al (1995) The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology 121 186 PMID: 8545524
Cooper et al (1994) GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg.Med.Chem.Lett. 4 1951
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Keywords: GR 159897, GR 159897 supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK, Receptor, 1274, Tocris Bioscience
4 Citations for GR 159897
Citations are publications that use Tocris products. Selected citations for GR 159897 include:
Kojima et al (2012) A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 167 1362 PMID: 22758653
Grant (2012) Tachykinins stimulate a subset of mouse taste cells. Cell Commun Signal 7 e31697 PMID: 22363709
Hegde et al (2010) Neurokinin-1 receptor antagonist treatment in polymicrobial sepsis: molecular insights. Int J Inflam 2010 601098 PMID: 21188216
Cunin et al (2011) The tachykinins substance P and hemokinin-1 favor the generation of human memory Th17 cells by inducing IL-1β, IL-23, and TNF-like 1A expression by monocytes. J Immunol 186 4175 PMID: 21368235
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