Background:

Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.

Volinanserin (MDL 100907) is a potent antagonist at the 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c receptor, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1].

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].

Reference：
[1]. Sorensen SM, et al. Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J Pharmacol Exp Ther. 1993 Aug;266(2):684-91.
[2]. Ardayfio PA, et al. The 5-hydroxytryptamine2A receptor antagonist R-(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat. J Pharmacol Exp Ther. 2008 Dec;327(3):891-7.