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.
Cooperet
al (1994) GR 159897 and related analogues as highly potent, orally active
non-peptide neurokinin NK2 receptor antagonists.
Bioorg.Med.Chem.Lett. 4 1951. Beresfordet al
(1995) GR 159897, a potent non-peptide antagonist at tachykinin NK2
receptors. Eur.J.Pharmacol. 272 241. Walshet 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.
