乙酰胆碱转运抑制剂，(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) 是一种有效的囊泡乙酰胆碱转运 (vesicular acetylcholine transport) 抑制剂，Ki 为 2 nM。(±)-Vesamicol hydrochloride 也对 σ1 和 σ2 受体具有高亲和力，Ki 值分别为 26 nM 和 34 nM。
中文名称
(±)-Vesamicol hydrochloride
中文别名
(±)-2-(4-苯基***基)环己醇盐酸盐;2-(4-苯基-1-***基)环己醇盐酸盐(1:1);2-羟甲基-5-氨基苯基硼酸
英文名称
(±)-Vesamicol hydrochloride
英文别名
Cyclohexanol,2-(4-phenyl-1-piperidinyl)-, hydrochloride (1:1), (1R,2R)-rel-;(+/-)-VESAMICOL HYDROCHLORIDE;(±)-Vesamicol hydrochloride;AH-5183;(+/-)-VESAMICOL HCL;AH-5183 HYDROCHLORIDE;(±)-VesamicolHCl (AH-5183);Ah-5183((+/-)-2-(4-phenylpiperidino) cyclohexanol;(+/-)-2-(4-PHENYLPIPERIDINO)CYCLOHEXANOL HYDROCHLORIDE;(±)-2-(4-Phenylpiperidino)cyclohexanol hydrochloride, AH-5183 hydrochloride;(+/-)-VESAMICOL HYDROCHLORIDE (AH-5183) >98%
Cas No.
120447-62-3
分子式
C17H25NO.HCl
分子量
295.85
包装储存
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.
性状
Solid
IC50 & Target[1][2]
Ki: 2 nM (Vesicular acetylcholine transport), 26 nM (σ1 receptors) and 34 nM (σ2 receptors)
体外研究(In Vitro)
The pharmacological actions of (±)-Vesamicol have been attributed to inhibition of acetylcholine transport into synaptic vesicles and the subsequent quantal release of acetylcholine.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(±)-Vesamicol (3 mg/kg; intraperitoneal injection; once; male Wistar rats) treatment increases the levels of cytosolic acetylcholine (ACh) in all regions of the brain, while those of vesicular ACh decreased in all regions except for the striatum.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male Wistar rats (120-300 g)
Dosage: 3 mg/kg
Administration: Intraperitoneal injection; once
Result: The levels of cytosolic acetylcholine (ACh) increased in all regions of the brain, while those of vesicular ACh decreased in all regions except for the striatum.
运输条件
Room temperature or refrigerated transportation.
储存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. S M Efange, et al. N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4-piperidine]: vesamicol analogues with affinity for monoamine transporters. J Med Chem. 1997 Nov 21;40(24):3905-14. [Information]
[2]. H Kobayashi, et al. Effects of systemic administration of 2-(4-phenyl-piperidino)-cyclohexanol (vesamicol) and an organophosphate DDVP on the cholinergic system in brain regions of rats. Brain Res Bull. 1997;43(1):17-23. [Information]
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