组织胺毒素增强激动剂诱导的乙酰胆碱受体脱敏。
Histrionicotoxin enhances agonist-induced desensitization of acetylcholine receptor.
作者信息
Burgermeister W, Catterall W A, Witkop B
出版信息
Proc Natl Acad Sci U S A. 1977 Dec;74(12):5754-8. doi: 10.1073/pnas.74.12.5754.
Abstract
Dihydroisohistrionicotoxin inhibits acetylcholine receptor-dependent 22Na+ uptake of cultured chick muscle cells with a KI of 0.2 micrometer. The inhibition is noncompetitive with respect to agonists. The toxin enhances desensitization of the receptor by agonists which is accompanied by a 10-fold increase in receptor affinity for agonists. Dihydroisohistrionicotoxin increases the affinity of the desensitized form of the receptor for agonists but not antagonists. The results suggest that dihydroisohistrionicotoxin inhibits the acetylcholine receptor by causing an increase in the affinity of the desensitized form of the receptor for agonists and thereby stabilizing the desensitized state.
摘要
二氢异组胺毒素抑制培养的鸡肌肉细胞中乙酰胆碱受体依赖性的22Na+摄取，其抑制常数（KI）为0.2微米。这种抑制作用对于激动剂而言是非竞争性的。该毒素增强了激动剂引起的受体脱敏作用，同时受体对激动剂的亲和力增加了10倍。二氢异组胺毒素增加了脱敏形式的受体对激动剂而非拮抗剂的亲和力。结果表明，二氢异组胺毒素通过增加脱敏形式的受体对激动剂的亲和力来抑制乙酰胆碱受体，从而稳定脱敏状态。
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