大鼠脑中毒蕈碱受体构型状态之间的转换。
Conversion between configurational states of the muscarinic receptor in rat brain.
作者信息
Aronstam R S, Hoss W, Abood L G
出版信息
Eur J Pharmacol. 1977 Dec 1;46(3):279-82. doi: 10.1016/0014-2999(77)90344-2.
Reductive alkylation of neural membranes by N-ethyl maleimide (NEM) converts muscarinic acetylcholine receptors from a state of low to high affinity for receptor agonists. Interactions of muscarinic antagonists with the receptor are unaffected by this treatment. Muscarinic receptors from the rat telencephalon in the high agonist affinity state are increased from 34.2 to 53.4% of the total receptor population and the Ki for carbamylcholine inhibition of 3-quinuclidinyl benzilate binding is decreased from 1.2 X 10(-4) to 6.9 X 10(-5) M by NEM treatment.
N - 乙基马来酰亚胺（NEM）对神经膜的还原烷基化作用可将毒蕈碱型乙酰胆碱受体从对受体激动剂低亲和力状态转变为高亲和力状态。毒蕈碱拮抗剂与该受体的相互作用不受此处理的影响。经NEM处理后，大鼠端脑处于高激动剂亲和力状态的毒蕈碱受体在总受体群体中的比例从34.2%增加到53.4%，并且氨甲酰胆碱抑制3 - 喹核啶基苯甲酸酯结合的Ki值从1.2×10⁻⁴ M降至6.9×10⁻⁵ M。
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