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烟碱型乙酰胆碱受体的离子通道无法区分全氢组氨毒素的旋光对映体。

The ionic channel of the nicotinic acetylcholine receptor is unable to differentiate between the optical antipodes of perhydrohistrionicotoxin.

作者信息

Spivak C E, Maleque M A, Takahashi K, Brossi A, Albuquerque E X

出版信息

FEBS Lett. 1983 Nov 14;163(2):189-93. doi: 10.1016/0014-5793(83)80816-3.

Abstract

The enantiomers of perhydrohistrionicotoxin were studied in their effects on endplate currents recorded at the junctional region of sartorius muscles of Rana pipiens. The two optical antipodes progressively decreased the peak amplitude of the endplate currents and were indistinguishable from each other at all times. The enantiomers shortened equally the time constants for endplate current decay, but did not alter their voltage sensitivities. Although perhydrohistrionicotoxin contains 4 chiral centers, complete steric inversion does not alter its effects on the acetylcholine receptor-ion channel complex. By contrast the recognition site of the AcChR is extremely sensitive to any change in the chirality of agonists.

摘要

研究了全氢组氨毒碱的对映体对牛蛙缝匠肌接头区记录的终板电流的影响。两种旋光对映体均逐渐降低终板电流的峰值幅度,且在所有时间点均无差异。对映体同样缩短了终板电流衰减的时间常数,但未改变其电压敏感性。尽管全氢组氨毒碱含有4个手性中心,但完全的空间反转并不改变其对乙酰胆碱受体-离子通道复合物的作用。相比之下,乙酰胆碱受体的识别位点对激动剂手性的任何变化都极其敏感。

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