0 CHa AChE Inhibitors(quaternary N-C-0 +N CHa HgC-NH-C- HgC CH3 alcohols and carbamates) Reversable (reversible non- Neostigmine Carbaryl covalent binding to the active 0 center of the enzyme): HgC CHa CHa C-O HO +N-C2Hs -Neostigmine, H CH3 -Physostigmine - Edrophonium, CHa CHa -Tacrin, Physostigmine Edrophonium Danopezil CH3CH3 HsC2-O、IⅡ +> CHg H3C-C-CH-O、I CP-S-CH2-CH2-N- CH3 P-F H5C2-0 CH3 Echothiophate Soman Irreversible(covalent binding to the active center of the enzyme): s HsC2-o、 Organophosphates P一( H5C2一0 → phosphorylation of the active center -Malathion Parathion Paraoxon -Parathion -Sarin Hac-ol Ecothiopate H3C-O -S-CH-C-O-C2H5→ CH2-C-O-C2H5 Malathion Malaoxon
AChE Inhibitors (quaternary alcohols and carbamates) Reversable (reversible noncovalent binding to the active center of the enzyme) : －Neostigmine, －Physostigmine , －Edrophonium , －Tacrin, －Danopezil Irreversible(covalent binding to the active center of the enzyme)： Organophosphates phosphorylation of the active center －Malathion －Parathion －Sarin －Ecothiopate
Reaction mechanism Direct-acting parasympathomimetic Indirect-acting parasympathomimetic (cholinergic drug) (cholinesterase drug) DD D D AChE ACh ACh ACh ACh mwowa-om ACh ACh ACh ACh D mwOwA-o m AChE A B DD Drugs that block the hydolysis of the esters are called cholinesterase inhibitor
Reaction mechanism Drugs that block the hydolysis of the esters are called cholinesterase inhibitor
The action of physostigmine(毒扁豆碱) ●Acetylcholine Acetylcholine .Choline Mascarnic s3ap4c Prosyartic mebn Mascarinic Synaptic cloft D威y四pt Choirv 风ytp ceptor Ncotinic ACh ace业e nceptor D城y国ptc cepOor AChE 印e的ane
The action of physostigmine (毒扁豆碱）