Chemical Name:3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolineca
rboxamide
Biological Activity:
Potent and selective non-peptide NK3 receptor
antagonist. Ki values are 4.4, >100,000 and 250 nM for human NK3,
NK1 and NK2 receptors respectively. Brain penetrant and
active in vivo.
Medhurstet al (1997) In vitro and in vivo
characterization of NK3 receptors in the rabbit eye by use of
selective non-peptide NK3 receptor antagonists. Br.J.Pharmacol. 122
469. Sarauet al (2000) Nonpeptide tachykinin receptor
antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a
central nervous system penetrant, potent and selective NK-3 receptor
antagonist. J.Pharmacol.Exp.Ther. 295 373. Sarauet al
(2000) Evidence that the proposed novel human “neurokinin-4” receptor is
pharmacologically similar to the human neurokinin-3 receptor but is not of
human origin. Mol.Pharmacol. 58 552.
