New Non-Competitive achEIs Exhibit greater CNS AChE CH,O CH N一cH selectivity CH,O Little or no hepatotoxicity Donepezil(多奈哌齐) CH CH 3 CH,O N o、N、CH3 CH3 CH3 Rivastigmine(利斯的明) Galantamine(加兰他敏)
New Non-Competitive AChEIs •Exhibit greater CNS AChE selectivity •Little or no hepatotoxicity
3.2 Anticholinergic Drugs(抗胆碱药) Muscarinic antagonists Nicotinic antagonists Neuromuscular blocking agents(N2 receptor)神经肌肉阻断剂 Ganglionic blocking agents(N1 receptor)神经节阻断剂
3.2 Anticholinergic Drugs （抗胆碱药） • Muscarinic antagonists • Nicotinic antagonists • Neuromuscular blocking agents (N2 -receptor)神经肌肉阻断剂 • Ganglionic blocking agents （N1 -receptor）神经节阻断剂
3. 2.1 Muscarinic antagonists Muscarinic antagonists are compounds that have high affinity for M-receptor but have no intrinsic activity Competitive(reversible) antagonists of ACh Antagonism responses include: decreased contraction of gi and urinary tract smooth muscles dilation of pupils(扩张瞳孔), reduced gastric secretion, decreased saliva(唾液) secretion
3.2.1 Muscarinic antagonists • Muscarinic antagonists are compounds that have high affinity for M-receptor but have no intrinsic activity. Competitive (reversible) antagonists of ACh •Antagonism responses include: decreased contraction of GI and urinary tract smooth muscles, dilation of pupils ( 扩 张 瞳 孔 ), reduced gastric secretion, decreased saliva （唾液）secretion
Therapeutic Uses of Muscarinic antagonists Treatment of smooth muscle spasms(肌痉挛) Ophthalmologic(眼科) examinations Treatment of gastric ulcers(胃溃疡) Reduction of nasal and upper respiratory tract secretions in cold and flu
Therapeutic Uses of Muscarinic antagonists • Treatment of smooth muscle spasms (肌痉挛) • Ophthalmologic （眼科） examinations • Treatment of gastric ulcers (胃溃疡) • Reduction of nasal and upper respiratory tract secretions in cold and flu
Solanaceous alkaloids(茄生物碱类) Found mainly in henbane(花烟草)( Hyoscyamus nige;莨菪属), deadl! 7 nightshade(龙葵属植物)( Atropa belladonna,颠茄), and jimson weed( Datura stramonium,曼陀罗 H3CN HaC CHOH CH2OH Atropine(阿托品) Scopolamine(东莨菪碱)
Solanaceous Alkaloids （茄生物碱类） Found mainly in henbane (花烟草) (Hyoscyamus niger,莨菪属), deadly nightshade (龙葵属植物) (Atropa belladonna, 颠 茄 ), and jimson weed (Datura stramonium，曼陀罗叶)