《药理学》课程PPT教学课件（Efferent Sys）06 cholinergic agonists

Cholinergic agonists

Cholinergic agonists

ANS:Autonomic nervous systemCNS:Centralnervous systemCholinoceptor:Acetylcholine receptorAdrenergic receptor:Noradrenergic receptorNreceptors:Nicotinic receptorsMreceptors:Muscarinic receptorsa-adrenoceptorareceptors:β-adrenoceptor:B receptors:ACh:AcetylcholineAChE:Acetylcholinesterase

ANS: Autonomic nervous system CNS: Central nervous system Cholinoceptor: Acetylcholine receptor Adrenergic receptor: Noradrenergic receptor N receptors: Nicotinic receptors M receptors: Muscarinic receptors α receptors: α-adrenoceptor ßreceptors: ß–adrenoceptor: ACh: Acetylcholine AChE: Acetylcholinesterase

NE orNA:NorepinephrineD:Dopamineacetyl coA: acetylcoenzymeACOMT:Catechol-O-methyltransferaseMAO:Monoamine oxidasePositiveinotropic:Strengthen the contractility of the myocardiumPositive chronotropic:Increasetherate of contraction

NE or NA: Norepinephrine D: Dopamine acetyl coA: acetylcoenzyme A COMT: Catechol-O-methyltransferase MAO: Monoamine oxidase Positive inotropic: Strengthen the contractility of the myocardium Positive chronotropic: Increase the rate of contraction

Chapter4Cholinergic agonistsI.overviewAcetylcholine,bethanecholDirect actingCarbachol,pilocarpineIndirect actingEdrophonium,neostigmineCholinergicPhysostigmine,pyridostigmine(reversible)agonistsEchothiophate,Indirect actingisoflurophate(irreversible)Reactivation ofpralidoxineacetylcholine esterase

Chapter 4 Cholinergic agonists I. overview Cholinergic agonists Direct acting Indirect acting (reversible) Indirect acting (irreversible) Acetylcholine,bethanechol Carbachol, pilocarpine Edrophonium, neostigmine Physostigmine,pyridostigmine Echothiophate, isoflurophate Reactivation of acetylcholine esterase pralidoxine

Cholinomimeticdrugsl.CholinoceporsagonistM-receptoragonist(pilocarpine)N-receptoragonist(nicotine2.Anticholinestease(neostigmine,organophosphate

Cholinomimetic drugs 1. Cholinocepors agonist M-receptor agonist (pilocarpine) N-receptor agonist (nicotine) 2. Anticholinestease (neostigmine, organophosphate)

1.muscarinicreceptors:M,receptors:CNS neurons, sympathetic postganglionic neuronsM,receptors:myocardium,smooth muscleM,receptors:exocrine glands,vessels of the smooth muscle andendothelium2.nicotinicreceptors:N, receptors: ganglia and adrenal medullaN, receptors: skeletal muscle neuromuscular end-plates

1.muscarinic receptors: M1 receptors: CNS neurons, sympathetic postganglionic neurons M2 receptors: myocardium,smooth muscle M3 receptors: exocrine glands,vessels of the smooth muscle andendothelium 2.nicotinic receptors: N1 receptors: ganglia and adrenal medulla N2 receptors: skeletal muscle neuromuscular end-plates

IIthe cholinergicneuronA.Neurtransmission at cholinergic neuronsCholinergic transmissionl.Synthesisofacetylcholine:cholineCholine+acetyl-CoAacetylcholineacetyltransterase2.Storageofacetylcholineinvesicles

II the cholinergic neuron A. Neurtransmission at cholinergic neurons Cholinergic transmission 1.Synthesis of acetylcholine: Choline+acetyl-CoA acetylcholine 2.Storage of acetylcholine in vesicles choline acetyltransterase

3.Releaseofacetylcholine(exocytosis):When an action potential arrives at the nerve ending,calcium channels in the presynaptic membrane open,causing an increase in the concentration ofintracellularcalcium.Elevated calciumlevelspromote the fusion of synaptic vesicles with the cellmembrane(presynapticmembrane)andrelease ofacetylcholineinto the synaptic cleft

3. Release of acetylcholine (exocytosis) : When an action potential arrives at the nerve ending, calcium channels in the presynaptic membrane open, causing an increase in the concentration of intracellular calcium. Elevated calcium levels promote the fusion of synaptic vesicles with the cell membrane(presynaptic membrane) and release of acetylcholine into the synaptic cleft

4.Bindingto receptor:Afterrelease from the presynaptic terminal, acetylcholine maybind to and activate an acetylcholine receptor(cholinoceptor)5.Degradationofacetylcholine:acetylcholinesteraseAchcholine+acetic acidthe half-life of acetycholinein the synapseis very short

4. Binding to receptor: After release from the presynaptic terminal, acetylcholine may bind to and activate an acetylcholine receptor(cholinoceptor). 5. Degradation of acetylcholine: Ach choline + acetic acid the half-life of acetycholine in the synapse is very short. acetylcholinesterase

PresynapticaxonPresynapticaxonAcetylcholineAcetylcholinesteraseReceptorPostsynapticcellU0006000Postsynapticcell乙酰胆碱酯酶对乙酰胆碱的水解

乙酰胆碱酯酶对乙酰胆碱的水解