传出总论要点分析.pptVIP

传出神经系统药物概论 Key concept Nerve — ENS Transmitter — ACh/NA Receptor Drug Autonomic（Vegetative）nervous system sympathetic nervous system parasympathetic nervous system Somatic motor nervous system 传出神经按递质分类 胆碱能神经 运动神经 所有节前纤维 副交感神经节后纤维 支配汗腺和骨骼肌血管 的交感神经节后纤维 去甲肾上腺素能神经 大多数交感神经节后纤维 Transmitter 1921: perfusion experiment in isolated toad hearts by Loewi →Implication of Ach 1946: identification of NA by Von Euler 乙酰胆碱受体（AChR） Muscarine AChR — MAChR M1; M2; M3; M4; M5 Nicotine AChR — NAChR NmAChR NnAChR 肾上腺素受体（Adrenoceptors） ? Adrenoceptors — ?1; ?2 ? Adrenoceptors — ?1; ?2; ?3 多巴胺能受体（Dopaminergic receptor） D1 —— peripheral effectors D2 —— presynaptic membrane MAChR 460～590 amino acid residues superfamily of G-protein-coupled receptors NAChR ligand-gated ion channel receptors Pentamer: 2a/b/g/d Adrenoceptors G-protein-coupled receptors a receptors coupled with different subGs b receptors coupled with same subG Act on receptors agonist blocker/antagonist Influence on transmitters release transport/storage transformation Drug —— Classification Agonists Antagonists 胆碱受体激动药 M, N receptor agonists (carbachol) M receptor agonists (pilocarpine) N receptor agonists (nicotine) 肾上腺素受体激动药 a adrenoceptor agonists a1, a2 adrenoceptor agonists (noradrenaline) a1 adrenoceptor agonists (phenylephrine) a2 adrenoceptor agonists (clonidine) b adrenoceptor agonists b1, b2- adrenoceptor agonists (isoprenaline) b1 adrenoceptor agonists (dobutamine) b2 adrenoceptor agonists (salbutamol) 胆碱受体阻断药 M receptor antagonists nonselective M receptor antagonists (atropine) selective M receptor antagonists M1 receptor antagonists (pirenzepine) M2 receptor antagonists（戈拉碘铵） M3 receptor antagonists (hexahydrosiladifenidol) N receptor antagonists Nn receptor antagonists (trimethaphan) Nm receptor antagonists (d-Tubocurarine) 肾上腺素受体阻断药 a adrenoceptor antagonists a1, a2 adrenoceptor antgonists short term