GR 159897

Cat. No. 1274

GR 159897 C23H27FN2O2S [158848-32-9]

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Chemical Name: 5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole

Biological Activity

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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M.Wt:
414.54
Formula:
C23H27FN2O2S
Solubility:
Soluble to 50 mM in DMSO and to 10 mM in ethanol
Purity:
>97 %
Storage:
Desiccate at -20°C
CAS No:
158848-32-9

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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.

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

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.

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.

Hegde et al (2010) Neurokinin-1 receptor antagonist treatment in polymicrobial sepsis: molecular insights. Int J Inflam 2010 601098. PMID: 21188216.

Do you know of a great paper that uses GR 159897 from Tocris? If so please let us know.

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Keywords: GR 159897, supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK, Tocris Bioscience, NK2 Receptor Antagonist products

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