Brestkin A P, Viniar T N, Rozengart E V
Biokhimiia. 1981 Jun;46(6):1042-8.
The effects of some ammonium compounds diiodomethylate acetate (I), propionate (II), butyrate (III), valeriate (IV) N-hydroxyethylanabasine, tetramethylammonium, tetraethylammonium and acetylcholine amide analog derivatives (V-VIII) on acetylthiocholine hydrolysis by cholinesterase from frog brain, acetylcholinesterase from human erythrocytes and butyryl cholinesterase from horse blood serum were studied. Cholinesterase from frog brain possesses a lower sensitivity to the inhibitors than does the mammalian enzyme. Significant conformational changes of the inhibitor molecule, i. e. transition from trans-conformation (V) to the fixed gosh-conformation (VII), have no effect on the anticholinesterase activity of these compounds. A method for evaluation of effectivity of different types of the reversible inhibitors is proposed.
研究了某些铵化合物二碘甲基乙酸酯（I）、丙酸酯（II）、丁酸酯（III）、戊酸酯（IV）、N-羟乙基假木贼碱、四甲铵、四乙铵以及乙酰胆碱酰胺类似衍生物（V - VIII）对蛙脑胆碱酯酶、人红细胞乙酰胆碱酯酶和马血清丁酰胆碱酯酶催化乙酰硫代胆碱水解的影响。蛙脑胆碱酯酶对这些抑制剂的敏感性低于哺乳动物酶。抑制剂分子的显著构象变化，即从反式构象（V）转变为固定的戈什构象（VII），对这些化合物的抗胆碱酯酶活性没有影响。提出了一种评估不同类型可逆抑制剂有效性的方法。
