C. Routledge et al., DIFFERENTIAL-EFFECTS OF WAY-100135 ON THE DECREASE IN 5-HYDROXYTRYPTAMINE RELEASE INDUCED BY BUSPIRONE AND NAN-190, European journal of pharmacology, 276(3), 1995, pp. 281-284
1-(2-Methoxyphenyl)-3-[(phthalimido)butyl] piperazine (NAN-190) and 8-
[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8- azaspiro[4.5]decane-7,9-
dione (buspirone) are 5-HT1A receptor partial agonists which decrease
5-hydrolrytryptamine (5-HT) release in vivo. In order to assess whethe
r these ligands decrease 5-HT release by stimulating 5-HT1A receptors
we examined the ability of the selective 5-HT1A receptor antagonist N-
tert-butyl 3-4-(2-methoxyphenyl) piperazin-1-yl-2-phenylpropanamide di
hydrochloride (WAY-100135) to block their inhibitory effects on 5-HT.
NAN-190 (0.1 mg/kg s.c.) and buspirone (1.0 mg/kg s.c.) significantly
decreased extracellular levels of 5-HT in hippocampal dialysates. WAY-
100135 (10.0 mg/kg s.c.) attenuated the effect of buspirone but had no
significant effect on the NAN-190-induced decrease in 5-HT release. T
hese data demonstrate that buspirone is an agonist at the somatodendri
tic 5-HT1A receptor but that the inhibitory effects of NAN-190 on 5-HT
release may be mediated via a mechanism other than, or in addition to
, 5-HT1A receptor agonism.