(S)-Volinanserin  (Synonyms: (S)-MDL100907; (S)-M 100907)

(S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT₂ receptor, with a K_i of 0.36 nM, and shows 300-fold selectivity for 5-HT₂ receptor over 5-HT_1c, alpha-1 and DA D₂ receptors. Volinanserin has antipsychotic activity.

Ki: 0.36 nM (5-HT₂ receptor)^[1]

Volinanserin (MDL 100907) 是 5-HT₂ 受体的有效拮抗剂，K_i 为 0.36 nM，对 5-HT₂ 的选择性为 300 倍。它对 5-HT₂ 受体的选择性是对 5-HT_1c 受体、α-1 和 DA D₂ 受体的 300 倍。 Volinanserin 具有抗精神病活性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) 显着降低 d-苯丙胺刺激的小鼠运动活性，ED₅₀ 为 0.3 mg/kg，但没有表现出明显的降低小鼠的基线运动活动。 Volinanserin 在大鼠中产生昏厥，ED₅₀ 为 10-50 mg/kg。Volinanserin 不会减少阿扑吗啡引起的刻板印象或引起大鼠僵住症^[1]。 Volinanserin (M100907) 与 MK-801 联合使用 (1 μg/kg)，可显着降低强化物，（10, 100 μg/kg）还通过腹膜内注射剂量依赖性拮抗大鼠中 MK-801 的破坏作用。Volinanserin (6.25 μg/kg) 可增强 DRL 72-s 方案大鼠中 Tranylcypromine (HY-17447) 的抗抑郁样作用，也增强 Desipramine (HY-B1272A) 的抗抑郁样作用^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

373.46

C₂₂H₂₈FNO₃

175673-57-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]