Chi M, Sun M
Institute of Pharmacology and Toxicology, Beijing, China.
Adv Exp Med Biol. 1995;363:65-73. doi: 10.1007/978-1-4615-1857-0_9.
Organophosphate and other ligands were examined for binding on the membrane-bond nicotinic receptor at three conformational states. Soman (pinacolyl methylphosphonofluoridate), sarin (isopropyl methylphosphonofluoridate, tabun (ethyl N-dimethylphosphoramidocyanidate) and phencyclidine did not show any effect on the binding of [25I]alpha-cobrotoxin to the nicotinic receptor. However, VX, O-ethyl-S-(2-diisopropylaminoethyl) methylphosphonothiolate, at concentrations higher than 10 umol/L exhibited profound inhibition on the equilibrium binding rates in a concentration-dependent manner. Agonist nicotine and antagonist d-tubocurarine also showed significant inhibitions.
研究了有机磷酸酯和其他配体在三种构象状态下与膜结合烟碱型受体的结合情况。梭曼（甲基膦酸频哪酯）、沙林（甲基膦酸异丙酯）、塔崩（N,N-二甲基氰基磷酸乙酯）和苯环己哌啶对[25I]α-银环蛇毒素与烟碱型受体的结合没有任何影响。然而，VX（O-乙基-S-(2-二异丙氨基乙基)甲基硫代膦酸酯）在浓度高于10 μmol/L时对平衡结合速率表现出浓度依赖性的显著抑制作用。激动剂尼古丁和拮抗剂d-筒箭毒碱也表现出显著的抑制作用。
