Volinanserin

Volinanserin is a potent and selective antagonist of 5-HT₂ receptor, with a K_i of 0.36 nM, and shows 300-fold selectivity for 5-HT₂ receptor over 5-HT_1c, alpha-1 and DA D₂ receptors. Volinanserin has antipsychotic activity. IC50 & Target:Ki: 0.36 nM (5-HT₂ receptor)^[1] In Vitro:Volinanserin (MDL 100907) is a potent antagonist at the 5-HT₂ receptor, with a K_i of 0.36 nM, and shows 300-fold selectivity for 5-HT₂ receptor over 5-HT_1c receptor, alpha-1 and DA D₂ receptors. Volinanserin has antipsychotic activity^[1]. In Vivo:Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) significantly decreases d-amphetamine-stimulated locomotor activity in mice, with an ED₅₀ of 0.3 mg/kg, but shows no obvious reduction in the base-line locomotor activity in mice. Volinanserin produces atalepsy with an ED₅₀ of 10-50 mg/kg in rats. Volinanserin does not reduces apomorphine-induced stereotypies or produces catalepsy in rats^[1]. Volinanserin (M100907) combined with MK-801 significantly decreases reinforcers at 1 μg/kg, but dose-dependently (10, 100 μg/kg) antagonizes the disruptive effect of MK-801 in rats via i.p. administration. Volinanserin (6.25 μg/kg) enhances the antidepressant-like action of desipramine in rats performing under a DRL 72-s schedule, and elevates the antidepressant-like effect of tranylcypromine^[2].