1、第 一 节胆 碱 酯 酶 胆碱酯酶 (cholinesterase， ChE) 乙酰胆碱酯酶 (acetylcholinesterase，AChE) relatively specific for acetylcholine rapid acetylcholine hydrolysis at cholinergic synapses 胆碱酯酶 (cholinesterase， ChE) 假性胆碱酯酶 (pseudocholinesterase) relatively low specificity for acetylcholine acetylcholine hydrolysis in pl
2、asma and many other tissues AChE 分布 分子组成同聚体异聚体AChE 水解过程 结合 裂解 水解AcetateAc-serine hydrolysedAcetyl-group transferredto serine-OHAcetylcholine bindsEsteratic site Anionic site第 二 节抗 胆 碱 酯 酶 药 (anticholinesterase agents) OO NOO Nneostigminecholinecarbamyl-serine hydrolysed(slow)acetyl-group transferred
3、 to serine-OHAChac-serine hydrolysed(fast) acetateNHONNHOHisSer GluCOONNHOHisSer GluCOONNHisSer GluCOONNHisSer GluCOONNHisSer GluCOONNHisSer GluCOOphospate transferred to-NOHreactivationAChEreactivateddyfloscarbamyltransferredto serine-OHno spontaneous hydrolysisesteraticsitephosphorylatedenzymepral
4、idoximeNNHOHisSer GluCOOOO NNNHisSer GluCOOOOON NOO OONNOONFPHO OPrOPrOPrOPrHO POHO NN OPrOPrHO PO HO NNONNOPHOOPrCABAChEanionicsiteOONNFig.8-1 The interactions of AChE with acetylcholine(A) , reversible anticholinesterase drugs (B) and irreversible anticholinesterase agents(C) .难逆性抗AChE药 易逆性抗AChE药anticholinesterase agents非共价结合的抑制药 依酚氯铵（edrophonium） 他克林（tacrine）多奈哌齐（donepezil）
