Ach is the natural agonist at the linical Chen Related compounds euro neuromuscular research Carbachol and related CH3 compounds are used Tubocurarine and other clinically for GI disorders CH3 related compounds glaucoma, salivary CH are used to paralyze gland malfunction, etc muscles during surgery acetyIcholinestc O CH3 CH3 OCH3 OH NH2-C-OCH2 CH2 H Carbachol CH3O OH H3C H D-Tubocurarine
17 Clinical Chemistry Ach is the natural agonist at the neuromuscular junction. Tubocurarine is the primary paralytic ingredient in curare. Tubocurarine competes with ACh for binding to receptor- but does not open the pore. So tubocurarine is a neuromuscular blocking agent. Tubocurarine and other, related compounds are used to paralyze muscles during surgery. Carbachol is a synthetic agonist not hydrolyzed by acetylcholinesterase. Carbachol and related compounds are used clinically for GI disorders, glaucoma, salivary gland malfunction, etc. Suberyldicholine is a synthetic neuromuscular agonist. Related compounds are useful in the neuroscience research
Anticholinesterase Agents Anticholinesterase(anti-ChE) agents inhibit acetylcholinesterase(乙酰胆碱酯 酶) >prolong excitation at the NMj
18 Anticholinesterase Agents ➢Anticholinesterase (anti-ChE) agents inhibit acetylcholinesterase （乙酰胆碱酯 酶） ➢prolong excitation at the NMJ
Anticholinesterase Agents 1. Normal ACh Choline Acetate aChE With anti-achE ACh Choline Acetate anti-ACht
19 1. Normal: ACh Choline + Acetate AChE 2. With anti - AchE: ACh Choline + Acetate anti - AChE Anticholinesterase Agents
Uses of anti-ChE agents > Clinical applications( Neostigmine,新斯的明, Physostigmine毒扁豆碱) ≯ insecticides( organophosphate有机磷酸酯) Nerve gas(eg. Sarin沙林,甲氟膦酸异丙酯。 种用作神经性毒气的化学剂)
20 Uses of anti-ChE agents ➢Clinical applications (Neostigmine, 新斯的明, Physostigmine毒扁豆碱) ➢Insecticides (organophosphate 有机磷酸酯) ➢Nerve gas (e.g. Sarin 沙林，甲氟膦酸异丙酯。 一种用作神经性毒气的化学剂))
Sarin comes in both liquid and gas forms a highly toxic and volatile nerve agent developed by Nazi scientists in Germany in the 1930s 500 times more toxic than cyanide (i 化物)gas
21 Sarin ➢ comes in both liquid and gas forms, ➢ a highly toxic and volatile nerve agent developed by Nazi scientists in Germany in the 1930s. ➢ 500 times more toxic than cyanide （氢 化物） gas