Chemical Name:1,2,3,6-Tetrahydro-1-[2-(2-naphthalenyl)ethyl]-4-[3-(tr
ifluoromethyl)phenyl]-pyridine hydrochloride
Biological Activity:
Orally active, full agonist at 5-HT1A
receptors. Binds rat 5-HT1A with high affinity (Ki = 2.0
nM) and is > 300-fold selective over other 5-HT receptor subtypes (IC50
> 650 nM). Increases motoneuron survival and promotes effects of NGF on
neurite outgrowth in vitro. Displays neurotrophic activity in several
neurodegenerative models in vivo.
Bachy et al
(1993) Biochemical and electrophysiological properties of SR 57746A, a new,
potent 5-HT1A receptor agonist. Fund.Clin.Pharmacol. 7 487. Fournier et al
(1993) Protective effects of SR 57746A in central and peripheral models of
neurodegenerative disorders in rodents and primates. Neuroscience 55
629. Duonget al (1999) Effect of the nonpeptide neurotrophic
compound SR 57746A on the phenotypic survival of purified mouse motoneurons.
Br.J.Pharmacol. 128 1385.
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
