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[可逆性抑制剂对乙酰胆碱酯酶活性中心功能部位反应能力的影响]

[Effect of reversible inhibitors on the reaction capacity of functional portions of the active center of acetylcholinesterase].

作者信息

Tonkopiĭ V D, Ardab'eva T V

出版信息

Biull Eksp Biol Med. 1978 Oct;86(10):441-4.

PMID:708873
Abstract

The effect of galanthamine, tacrine, and oxazyl (ambenomum) on human red cells acetylcholinesterase phosphorylation by armine and Gd-42 (o-ethyl-s-beta-ethylthioethyl ester of methylthiophosphinic acid) was studied. In the presence of galanthamine phosphororganic inhibitors interacted only with the active center of the enzyme, the anionic site of which was not occupied by the reversible inhibitor. Tacrine and oxazyl decreased the reactivity of the free enzyme and the rate of its phosphorylation.

摘要

研究了加兰他敏、他克林和奥沙唑(氨苯那明)对人红细胞乙酰胆碱酯酶被氨胺和Gd-42(甲基硫代次膦酸的邻乙基-s-β-乙硫基乙酯)磷酸化的影响。在加兰他敏存在的情况下,有机磷抑制剂仅与酶的活性中心相互作用,其阴离子部位未被可逆抑制剂占据。他克林和奥沙唑降低了游离酶的反应性及其磷酸化速率。

相似文献

1
[Effect of reversible inhibitors on the reaction capacity of functional portions of the active center of acetylcholinesterase].[可逆性抑制剂对乙酰胆碱酯酶活性中心功能部位反应能力的影响]
Biull Eksp Biol Med. 1978 Oct;86(10):441-4.
2
[Interaction of reversible inhibitors with the catalytic centers and allosteric sites of cholinesterases].
Biull Eksp Biol Med. 1976 Aug;82(8):947-50.
3
[The effect of pH and reversible inhibitors on decarbamylation of acetylcholinesterase].
Ukr Biokhim Zh (1978). 1991 May-Jun;63(3):29-35.
4
Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities.
Mol Pharmacol. 1992 May;41(5):937-42.
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[Galanthamine interaction with mouse brain acetylcholinesterase in in vivo experiments].[加兰他敏在体内实验中与小鼠脑乙酰胆碱酯酶的相互作用]
Biull Eksp Biol Med. 1976 Jul;82(7):823-5.
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Altered binding of thioflavin t to the peripheral anionic site of acetylcholinesterase after phosphorylation of the active site by chlorpyrifos oxon or dichlorvos.在毒死蜱氧磷或敌敌畏使活性位点磷酸化后,硫黄素t与乙酰胆碱酯酶外周阴离子位点的结合发生改变。
Toxicol Appl Pharmacol. 2008 Aug 1;230(3):390-6. doi: 10.1016/j.taap.2008.03.006. Epub 2008 Mar 15.
7
[On the molecular mechanism of action of galanthamine, an antagonist of nondepolarizing muscle relaxants (author's transl)].[关于加兰他敏(非去极化肌松药拮抗剂)的分子作用机制(作者译)]
Anaesthesist. 1976 Sep;25(9):444-8.
8
Neuroprotective effects of galanthamine and tacrine against glutamate neurotoxicity.加兰他敏和他克林对谷氨酸神经毒性的神经保护作用。
Eur J Pharmacol. 2006 Nov 7;549(1-3):19-26. doi: 10.1016/j.ejphar.2006.08.017. Epub 2006 Aug 23.
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Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.亚烷基连接的他克林二聚体与加州电鳐乙酰胆碱酯酶的复合物:双5-他克林的结合导致活性位点峡谷发生显著重排。
J Med Chem. 2006 Sep 7;49(18):5491-500. doi: 10.1021/jm060164b.
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Toxicol In Vitro. 2006 Sep;20(6):824-31. doi: 10.1016/j.tiv.2006.01.002. Epub 2006 Feb 10.