R&D Systems Inc. Tocris Bioscience Boston Biochem

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.

Certificate of Analysis / Safety Data Sheet

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

References

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.

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.

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

View Related Products by Target

Keywords: GR 159897, supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK

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