139290-65-6
| 中文名称 | 139290-65-6 |
|---|---|
| 中文同义词 | Volinanserin MDL 100907 (R构型）;VOLINANSERIN MDL 100907 (R构型);氟利色林;诺和灵 M100907;(R)-(2,3-二甲氧基苯基)(1-(4-氟苯乙基)哌啶-4-基)甲醇 |
| 英文名称 | (R)-(+)-ALPHA-(2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUORO-PHENYL)ETHYL]-4-PIPERIDINE METHANOL |
| 英文同义词 | (+)-a-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol;(aR)-a-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol;M 100907;R-MDL 100907;(R)-(+)-(-(2,3-Dimethoxyphenyl)-1-[2-(4-fluoro-phenyl)ethyl]-4-piperidine methanol (R,R)-tartrate;4-Piperidinemethanol, 1-[2-(4-fluorophenyl)ethyl]-(-(2,3-dimethoxyphenyl)-, ((R), (R,R)-tartrate;MDL100907-L-tartrate;(R)-(+)-(-(2,3-Dimethoxyphenyl)-1-[2-(4-fluoro-phenyl)ethyl]-4-piperidine methanol |
| CAS号 | 139290-65-6 |
| 分子式 | C22H28FNO3 |
| 分子量 | 373.46 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 139290-65-6.mol |
| 结构式 |  |
139290-65-6 性质
| 熔点 | 89-91°C |
|---|---|
| 沸点 | 499.4±45.0 °C(Predicted) |
| 密度 | 1.150±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥20mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | 13.93±0.20(Predicted) |
| 颜色 | 灰白色至浅棕色 |
| Target | Value |
|
5-HT2 receptor
(Cell-free assay) | 0.36 nM(Ki) |
Volinanserin (MDL 100907) is a potent antagonist at the 5-HT 2 receptor, with a K i of 0.36 nM, and shows 300-fold selectivity for 5-HT 2 receptor over 5-HT 1c receptor, alpha-1 and DA D 2 receptors. Volinanserin has antipsychotic activity.
Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) significantly decreases d-amphetamine-stimulated locomotor activity in mice, with an ED 50 of 0.3 mg/kg, but shows no obvious reduction in the base-line locomotor activity in mice. Volinanserin produces atalepsy with an ED 50 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.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-14940 | Volinanserin | 1 mg | 500元 | |
| 2024/01/25 | HY-14940 | 139290-65-6 Volinanserin | 139290-65-6 | 5mg | 1100元 |