⑧ 上游充通大￥ SHANGHAI JIAO TONG UNIVERSITY 1896 1920 1987 2006 强 Chapter 6 Adrenoceptor drugs agonists and antagonists) 2产7AII7A00C7I/m-、. 。自。。 1Eg三
1896 1920 1987 2006 Chapter 6 Adrenoceptor drugs （ agonists and antagonists ）
⑧ Sympathetic pathway Cholinergic nicotinic receptor ACh Adrenergic receptor(a or b) Adrenergic postganglionic neuron Cholinergic Autonomic CNS preganglionic ganglion NE Target neuron tissue Parasympathetic pathway Cholinergic nicotinic receptor Cholinergic postganglionic Cholinergic muscarinic receptor neuron Cholinergic ACh CNS preganglionic Autonomic ACh Target neuron ganglion tissue
-A.Adrenergic transmission 3 Activates Adrenal Inhibits medulla Epinephrine(E) 0 Norepinephrine L-tyrosine Varicosities Bloodstream NE) L-dop阳 B-adrenoceptor Inactivated 2 (MAO) 1.Tyrosine hydroxylase Dopamine CAMP Action potential 2.Adenylyl cyclase PKA NE 6d 3.ATP,substance P az-adrenoceptor a2-adreno- ceptor Heart,glands. 4.Calcium channel smooth musde 6c 6b Inactivated: Re absorption by MAo by COMT Norepinephrine Epinephrine (NE) Capillary 6a Diffusion into blood (raises NE in blood) 0- adrenoceptors adrenoceptors P
Norepinephrine (NE) 1.Tyrosine hydroxylase 2.Adenylyl cyclase 3.ATP, substance P 4.Calcium channel
ADRENOCEPTORS C, B B: Inhibitionof Vasoconstriction norepinephrine -Tachycardia Vasodilation release nrsed periphera polysis Decreased peripheral resistance eS由(e nhibitionofactychoin release n myocardia Bronchodilation nreasedblood pressure onr时y Increased musde inhibition of ydi怕as站 casdeleas andwggyogenoysh insulin release of renin Increased release ofgluagn intemasphincter of the bladder Reaxedutri smooth musce
B.Adrenoceptors ⑧ Norepinephrine Natural agonists Epinephrine Agonists: Phenylephrine Clonidine Iso- Salbu- proterenol tamd Antagonists: Prazosin Yohimbine Atenolol Adrenergic receptors: 2 3 Go G, 4 B2 G CAMP CAMP↑ PLCp DAG PKA↑ PK↑ PKC PKA 公 当+a Hyper- Dolartzation [Ca2*] [Ca2*3↓ Hyper- polartzation [Ca2*]h↑ Inhibition of gastrointestinal motility Inhibition of d2 B2 01 exocytosis Drives heart Dilatation of Contraction of d orsecretion ·Vessels ·Blood vessels Salivary glands Bronchioles Bronchioles 。Insulin Uterus Sphincters ·Norepinephrine Renin release etc. Uterus ·Acetylcholine etc. etc