MDL 100907

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors; demonstrates a clozapine-like profile of potential antipsychotic activity with low extrapyramidal sid-effect liability, and has a superior CNS safety index.Sleep Disorder Phase 3 Discontinued (In Vitro) :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. (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. 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.

139290-65-6

MDL-100907 | MDL100907 | Volinanserin

>98% (HPLC)

DMSO: 100 mg/mL (267.8 mM) ; Ethanol: 18 mg/mL (48.2 mM) (< 1 mg/ml refers to the product slightly soluble or insoluble)

O[C@@H] (C1=CC=CC (OC) =C1OC) C2CCN (CCC3=CC=C (F) C=C3) CC2

C22H28FNO3

373.46

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.