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维生霉素的药理学:一种囊泡型乙酰胆碱转运体抑制剂。

The pharmacology of vesamicol: an inhibitor of the vesicular acetylcholine transporter.

作者信息

Prior C, Marshall I G, Parsons S M

机构信息

Department of Physiology and Pharmacology, University of Strathclyde, Royal College, Glasgow, Scotland.

出版信息

Gen Pharmacol. 1992 Nov;23(6):1017-22. doi: 10.1016/0306-3623(92)90280-w.

DOI:10.1016/0306-3623(92)90280-w
PMID:1487110
Abstract
  1. Vesamicol (2-[4-phenylpiperidino] cyclohexanol) inhibits the transport of acetylcholine into synaptic vesicles in cholinergic nerve terminals. 2. Recent pharmacological studies of the effects of vesamicol on skeletal neuromuscular transmission have revealed a pattern of activity for the compound consistent with the neurochemical observation of the mechanism of action of the compound. 3. Pharmacological manipulation of vesicular acetylcholine transport has been used to investigate the recycling and mobilization of synaptic vesicles within cholinergic nerve terminals. 4. In addition to its effects on vesicular acetylcholine transport, vesamicol also possesses some sodium channel and alpha-adrenoceptor blocking activity. 5. Vesamicol clearly represents a unique tool for investigating presynaptic mechanisms in cholinergic nerve terminals.
摘要
  1. 维生米可(2-[4-苯基哌啶基]环己醇)抑制胆碱能神经末梢中乙酰胆碱向突触小泡的转运。2. 近期关于维生米可对骨骼肌神经肌肉传递影响的药理学研究揭示了该化合物的一种活性模式,这与对该化合物作用机制的神经化学观察结果一致。3. 对囊泡乙酰胆碱转运的药理学操作已被用于研究胆碱能神经末梢内突触小泡的再循环和动员。4. 除了对囊泡乙酰胆碱转运的影响外,维生米可还具有一些钠通道和α-肾上腺素能受体阻断活性。5. 维生米可显然是研究胆碱能神经末梢突触前机制的一种独特工具。

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