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Volinanserin

CAS No. : 139290-65-6

MCE 国际站：Volinanserin

产品活性：Volinanserin 是一种有效的，选择性的 5-HT₂ 受体拮抗剂，K_i 值为 0.36 nM，对其选择性是对 5-HT_1c，alpha-1 和 DA D₂ 受体的 300 倍，可用于精神疾病的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

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.

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.

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