Shataeva G A, Makhaeva G F, Iankovskaia V L, Sokolov V B, Ivanov A N
Zh Evol Biokhim Fiziol. 1988 Nov-Dec;24(6):791-6.
Studies have been made on the interaction of four types of phosphorylated alkylchloroformoximes, i.e. analogues of an insecticide-acaricide valexon, with acetylcholinesterases from human erythrocytes and from the heads of the housefly Musca domestica. Antiacetylcholinesterase activity of the drugs depended both on the structure of the organophosphorus compounds, and the origin of the enzyme, indicating the existence of differences in the active surface of these acetylcholinesterases. Incorporation of one or two chloride atoms into alkylchloroformoxime group of the cleaved part of the organophosphorus compounds increased anticholinesterase activity with respect to both enzymes. Diethyl derivatives of these drugs exhibited higher specificity with respect to housefly enzyme as compared to human acetylcholinesterase.
已经对四种类型的磷酸化烷基氯代肟进行了研究，即杀虫剂杀螨剂伐力松的类似物，它们与人红细胞和家蝇头部的乙酰胆碱酯酶相互作用。这些药物的抗乙酰胆碱酯酶活性既取决于有机磷化合物的结构，也取决于酶的来源，这表明这些乙酰胆碱酯酶的活性表面存在差异。在有机磷化合物裂解部分的烷基氯代肟基团中引入一个或两个氯原子会增加对这两种酶的抗胆碱酯酶活性。与人类乙酰胆碱酯酶相比，这些药物的二乙基衍生物对家蝇酶表现出更高的特异性。
