沒(méi)有幻燈片標(biāo)題-浙江大學(xué)教學(xué)信息化平臺(tái)

1、Section XThe nervous system,Chapter 5Drugs Affecting the Nervous System,Part 1The Efferent Nervous System,Neurotransmitters and receptorsDrug actions and classification,,,Sympatheticnerves,Parasympatheticnerves,M

2、otor nerve,Overview of efferent nervous system,Autonomic nervous system,Sympathetic,Parasympathetic,Somatic motor nervous system,Ganglia,ACh,NEACh,ACh,Motor nerves,ACh,,,,,,,Chemical transmission via synapse,Overview o

3、f autonomic nervous system,Overview of autonomic nervous system,Synapse,Neurotransmitters,,,Receptors,Two types of acetylcholine receptors,Cholinoceptors,G protein-coupled receptor,Ion channel,Adrenoceptors: G protein-co

4、upled receptors,G protein-coupled receptor,,,,Termination of neurotransmitter actions,Neurotransmitter transporters,Enzymatic degradation: acetylcholinesterase,,1 Transmitters and Receptors,1.1 Transmitters(1) Acetyl

5、choline (ACh)Cholinergic nerves a. pre-ganglionic fibers of sympathetic and parasympathetic nerves b. post-ganglionic fibers of parasympathetic, and part of sympathetic nerves c. motor nerves,A Transmitter

6、s and Receptors,Acetylcholinesterase (AChE) Terminating ACh effects,,AChE,(2) Norepinephrine (NE) or noradrenaline (NA) Adrenergic nerves most of post-ganglionic fibers of sympathetic nerves,A Transmitte

7、rs and Receptors,,,,,,,,,Termination of norepinephrine effects Uptake neurotransmitter transporters uptake 1: neuronal uptake uptake 2: non-neuronal uptake Enzymatic degradation monoamine oxidase (M

8、AO) catechol-O-methyltransferease (COMT),A Transmitters and Receptors,Neurotransmitter transporters,,,,,2 Receptors2.1 Acetycholine receptors (cholinoceptors, cholinergic receptors) Muscarinic rec

9、eptors (M receptors) Nicotinic receptors (N receptors),A Transmitters and Receptors,Nicotinic receptors:ligand-gated ion channel,Mucarinic receptors:7-transmembrane G protein-coupled receptor,Mucarinic receptors

10、Depression of the heart: heart rate, conductionContraction of smooth muscles: sensitive: GI tract, bronchial, urinary bladder insensitive: uterine, blood vesselsExocrine glands: sensitive: sweat, tears, s

11、alivary insensitive: GI tractEye: miosis: contraction of sphincter muscle of iris contraction for near vision: contraction of ciliary muscle,A Transmitters and Receptors,N

12、icotinic receptorsNN receptors（ N1 receptors ） Sympathetic and parasympathetic ganglia Adrenal medullaNM receptors （N2 receptors ） Contraction of skeletal muscles,A Transmitters and Receptors,2.2 Adreno

13、ceptors (adrenergic receptors)? receptors?1 receptors: contraction of vascular smooth muscles: BP↑ contraction of radial muscle of iris: mydriasis?2 receptors: CNS, presynaptic membranes of adrenergic ner

14、ves: vasodilatation,A Transmitters and Receptors,? receptors?1 receptors: contractility, automaticity, conduction, oxygen-consumption, cardiac output: heart stimulation?2 receptors: relaxation of bronchial smooth

15、muscles,B Transmitters and Receptors,B Drug actions and classification,1. Mechanisms of drug actions1.1 Direct actions on the receptors Agonists Antagonists,B Drug actions and classification,1.2 Indirect

16、actions via affecting transmitters (1) Synthesis: L-dopa 左旋多巴 (2) Inactivation: AChEI, MAOI (3) Release: neostigmine 新斯的明, ephedrine 麻黃堿, amphetamine 苯丙胺 (4) Transport and storage: imipramine

17、丙咪嗪, reserpine 利血平（利舍平）,1.3 Mimetics and antagonists (1) Mimetics direct-acting: receptor agonists indirect-acting: increasing amounts and/or effects of transmitters (2) Antagonists direct-actin

18、g: receptor antagonists indirect-acting: decreasing amounts and/or effects of transmitters,B Drug actions and classification,2. Drug classification2.1 Cholinomimetics (1) Cholinoceptor agonists M, N rece

19、ptor agonists: carbachol 卡巴膽堿 M receptor agonists: pilocarpine 毛果蕓香堿 N receptor agonists: nicotine 煙堿 (2) Cholinesterase inhibitors (Anticholinesterases) Reversible: neostigmine 新斯的明 Irreversible: o

20、rganophosphates 有機(jī)磷酸酯類(lèi),B Drug actions and classification,2.2 Cholinergic antagonists(1) Cholinoceptor antagonistsM cholinoceptor antagonists non-selective: atropine 阿托品 M1 cholinoceptor-selective: parenzep

21、ine 哌侖西平,B Drug actions and classification,N cholinoceptor antagonists NN cholinoceptor antagonists: mecamylamine

22、 美加明 NM cholinoceptor antagonists: succinylcholine 琥珀膽堿(2) Cholinesterase reactivators pralidoxime iodide 碘解磷定,B Drug actions and classificati

23、on,2.3 Adrenoceptor agonists(1) ? receptor agonists ?1?2 receptor agonists: norepinephrine 去甲腎上腺素?1 receptor agonists: phenylephrine 去氧腎上腺素?2 receptor agonists: clonidine 可樂(lè)定(2) ?, ? receptor agonists e

24、pinephrine, adrenaline 腎上腺素,B Drug actions and classification,(3) ? receptor agonists：?1?2 receptor agonists: isoproterenol 異丙腎上腺素?1 receptor agonists: dobutamine 多巴酚丁胺?2 recep

25、tor agonists: salbutenol 沙丁胺醇,B Drug actions and classification,2.4 Adrenoceptor antagonists（1）? receptor antagonists?1?2 receptor antagonists: short-acting: phentolamine 酚妥拉明 long-acting: phenoxybenzamine

26、酚芐明?1 receptor antagonists: prazosin 哌唑嗪?2 receptor antagonists: yohimbine育亨賓,B Drug actions and classification,（2）? receptor antagonists?1?2 receptor antagonists: propranolol 普萘洛爾?1 receptor antagonists: atenolol