Cat. No. 1274
Chemical Name: 5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
Biological ActivityA 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 InformationSold with the permission of GlaxoSmithKline
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
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.
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Keywords: GR 159897, supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK
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