胃复安的间接parasympathomimetic活动:可逆抑制胆碱酯酶从人类中枢神经系统和血液。
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Chemnitius JM, Haselmeyer KH、Gonska BD Kreuzer H,泽赫R
胃复安的间接parasympathomimetic活动:可逆抑制胆碱酯酶从人类中枢神经系统和血液。
药物杂志》1996 Jul-Aug; 34 (1 - 2): 65 - 72。
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8981558 (在PubMed]
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多巴胺的抑制效应D2-receptor对抗苯甲酰胺化合物胃复安(MCP)对乙酰胆碱酯酶(疼痛;EC 3.1.1.7)同功酶红细胞和人类的尾状核和对人类血清胆碱酯酶(ChE);EC 3.1.1.8)研究了体外使用分光光度测定acetylthiocholine (ASCh)作为衬底。MCP在化验浓度变化从0.30 microM 0.15毫米。所有同功酶浓度的方式被胃复安抑制进行了研究。MCP抑制疼痛格瓦拉同功酶并没有时间和可逆的类型。双倒数的情节对不同浓度ASCh透露,反应速度,疼痛同功酶的红细胞和尾状核,MCP减少两个最大反应速度(Vmax)和底物亲和力(明显的米氏常数,公里,增加)。因此,MCP抑制疼痛的同功酶的混合竞争/非竞争性类型。MCP常数为可逆的竞争性(Ki)和非竞争性(Ki)可以确定抑制红细胞疼痛(Ki = 10 microM;Ki = 70 microM)和尾状核疼痛(Ki = 9.3 microM;Ki = 82 microM)。 In contrast to MCP inhibition of AChE isoenzymes, the type of reversible MCP inhibition of human serum ChE depended on substrate concentration. If substrate concentration exceeded 0.2 mM, MCP inhibition was of mixed competitive/non-competitive type (Ki = 0.19 microM; Ki = 1.4 microM). MCP inhibition was of uncompetitive type, if substrate concentration was below 0.2 mM (Ki(u) = 1.0 microM). The mixed-type MCP inhibition of cholinesterase isoenzymes, because of its non-competitive component, can only partially be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Since, with intravenous infusions, peak MCP plasma concentrations in humans reach 4 microM, MCP inhibition of ACh hydrolysis in vivo may contribute both to prokinetic and anti-emetic actions of the substance and to its extrapyramidal side effects.