Chemical Name:1-[[(2-Nitrophenyl)amino]carbonyl]-L-prolyl-N-methyl-3-
(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
Biological Activity:
Highly selective human tachykinin NK1
receptor antagonist (IC50 values are 0.62 and 451 nM for human and
rat receptors respectively) that displays > 130-fold selectivity over human
NK2 and NK3 receptors. Potently antagonises SP-induced Ca2+
efflux in vitro and inhibits mechanical hyperalgesia in vivo.
Walpoleet
al (1998) Comparative, general pharmacology of SDZ NKT 343, a novel,
selective NK1 receptor antagonist. Br.J.Pharmacol. 124 83. Walpoleet al (1998) 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N-methylamide
(SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist
with good oral analgesic activity in chronic pain models. J.Med.Chem. 41
3159. Campbellet al (1998) Selective neurokinin-1 receptor
antagonists are anti-hyperalgesic in a model of neuropathic pain in the
guinea-pig. Neuroscience. 87 527.