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κ-银环蛇毒素与牛嗜铬细胞烟碱型受体的相互作用。

The interaction of kappa-bungarotoxin with the nicotinic receptor of bovine chromaffin cells.

作者信息

Nooney J M, Lambert J J, Chiappinelli V A

机构信息

Department of Pharmacology and Clinical Pharmacology, Ninewells Hospital, University of Dundee, U.K.

出版信息

Brain Res. 1992 Feb 21;573(1):77-82. doi: 10.1016/0006-8993(92)90115-p.

Abstract

Whole-cell recording techniques were used to examine acetylcholine-induced nicotinic currents in isolated bovine chromaffin cells. The effects on these currents of kappa-bungarotoxin, a snake venom kappa-neurotoxin, were tested. Exposure of cells to kappa-bungarotoxin (600 nM for 40 min) produced a prolonged blockade of nicotinic currents. The mechanism of this blockade was examined in several ways. Firstly, the pre-exposure of cells to trimetaphan, a competitive nicotinic antagonist, protected against the action of subsequent additions of kappa-bungarotoxin. Secondly, voltage-clamp measurements indicated that the degree of blockade produced by kappa-bungarotoxin was independent of cell membrane potential. Unlike (+)-tubocurarine, kappa-bungarotoxin had no direct agonist effects on nicotinic receptors. It is concluded from the present functional studies and from previously reported binding studies that kappa-bungarotoxin blocks nicotinic responses in bovine chromaffin cells by binding to regions overlying acetylcholine sites on nicotinic receptors.

摘要

采用全细胞记录技术检测分离的牛嗜铬细胞中乙酰胆碱诱导的烟碱样电流。测试了蛇毒κ-神经毒素κ-银环蛇毒素对这些电流的影响。将细胞暴露于κ-银环蛇毒素(600 nM,持续40分钟)会导致烟碱样电流的长期阻断。通过几种方式研究了这种阻断的机制。首先,将细胞预先暴露于竞争性烟碱样拮抗剂曲美芬,可防止随后添加κ-银环蛇毒素的作用。其次,电压钳测量表明,κ-银环蛇毒素产生的阻断程度与细胞膜电位无关。与(+)-筒箭毒碱不同,κ-银环蛇毒素对烟碱样受体没有直接激动作用。从目前的功能研究和先前报道的结合研究得出结论,κ-银环蛇毒素通过结合烟碱样受体上乙酰胆碱位点上方的区域来阻断牛嗜铬细胞中的烟碱样反应。

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