MDL 100907

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 5-HT2A 受体拮抗剂，Ki 为 0.36 nM，对 5-HT2A 的选择性是其他血清素受体的 80 倍以上。

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.

——

——

MDL-100907 | MDL100907 | Volinanserin

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Neurological Disease

Sleep Disorder

139290-65-6

373.46

C22H28FNO3

>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

(R)-(+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperinemethanol

(-20℃)

With Ice Pack

≥ 2 years