(-)-MDL 100907

Product Name(-)-MDL 100907
CAS175673-57-1
MFC22H28FNO3
MW373.465
EINECS
MOL File175673-57-1.mol

Chemical Properties

Boiling point	499.4±45.0 °C(Predicted)
Density	1.150±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	Ethanol: Soluble: =10 mg/ml
pka	13.93±0.20(Predicted)

Usage And Synthesis

Uses

(S)-Volinanserin is an isform of Volinanserin (HY-14940). 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.

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 (HY-B1272A) in rats performing under a DRL 72-s schedule, and elevates the antidepressant-like effect of Tranylcypromine (HY-17447)^[2].

References

[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. PMID:8102646
[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. DOI:10.1124/jpet.108.143370
[3] TIMO HEINRICH DR. 1-(1-Phenethylpiperidin-4-yl)-1-phenylethanols as Potent and Highly Selective 5-HT2A Antagonists[J]. ChemMedChem, 2006, 1 2: 245-255. DOI: 10.1002/cmdc.200500023

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