Balashova E K, Brestkin A P, Vikhreva L A, Godovikov N N, Kabachnik M I
Zh Evol Biokhim Fiziol. 1982 Jul-Aug;18(4):325-9.
Studies have been made of the effect of organophosphorus inhibitors (OPI) containing butynilic group in the detectable part of the molecule, and of their saturated analogues on cholinesterases from different species of mammals and arthropods. In all cases without a single exception, acetylene compounds exhibited higher anticholinesterase effect than saturated ones. The value of "acetylene effect" varied to a great extent and depended on both the structure of OPI and the source of cholinesterase, these data indicating the existence of differences in the structure of the active site in cholinesterases investigated. The acetylene effect was always higher in ethylmercapto-substituted OPI than in chloride-substituted ones. Among thiophosphates, the highest (7,600) effect was found for cholinesterase of the spider mite in the case of dimethyl esters. Among thiophosphonates, exceptionally high (38,000) effect was noted for cholinesterase from the head of the domestic fly when methylthiophosphonates were compared. In this pair of compounds, the inhibitory constant k2 for the cholinesterase of the fly by acetylene derivative was equal to 1.1 . 10(9).
已经对分子可检测部分含有丁炔基的有机磷抑制剂（OPI）及其饱和类似物对不同种类哺乳动物和节肢动物胆碱酯酶的影响进行了研究。在所有情况下无一例外，乙炔化合物表现出比饱和化合物更高的抗胆碱酯酶作用。“乙炔效应”的值在很大程度上有所不同，并且取决于OPI的结构和胆碱酯酶的来源，这些数据表明所研究的胆碱酯酶活性位点的结构存在差异。乙炔效应在乙硫基取代的OPI中总是高于氯取代的OPI。在硫代磷酸酯中，对于二甲基酯，红蜘蛛胆碱酯酶的效应最高（7600）。在硫代膦酸酯中，当比较甲硫代膦酸酯时，家蝇头部胆碱酯酶的效应异常高（38000）。在这对化合物中，乙炔衍生物对家蝇胆碱酯酶的抑制常数k2等于1.1×10⁹。
