《药理学》课程PPT教学课件(Efferent Sys)10 adrenergic agonists

theadrenergic agonistsI.overviewThe adrenergic drugs affect receptors thatare stimulated by norepinephrine orepinephrine. Some adrenergic drugs actdirectly on the adrenergic receptoradrenoceptor) by activating it and aresaid to be sympathomimetic
the adrenergic agonists I. overview The adrenergic drugs affect receptors that are stimulated by norepinephrine or epinephrine. Some adrenergic drugs act directly on the adrenergic receptor (adrenoceptor) by activating it and are said to be sympathomimetic

Direct-actingAlbuterol clonidinedobutaminedopamineEpinephine isoproterenol metaproterenolMethoxamine norepinephrine phenylephrineAdrenergicRitodrine terbutalineagonistsIndirect-actingAmphetaminetyramineDirectandindirectactingEphedrine metaraminol
Adrenergic agonists Direct-acting Albuterol clonidine dobutamine dopamine Epinephine isoproterenol metaproterenol Methoxamine norepinephrine phenylephrine Ritodrine terbutaline Indirect-acting Amphetamine tyramine Ephedrine metaraminol Direct and indirect acting

IIThe adrenergicneuronA.neurotransmission at adrenergic neurons:1.Synthesis ofnorepinephrine:DopaTyrosineDopaTyrosineDopaminehydroxylasedecarboxylasedopaminenorepinephrineepinephrineN-methyltransferaseβ-hydroxylase
1.Synthesis of norepinephrine: Tyrosine Dopa Tyrosine Dopa Dopamine hydroxylase decarboxylase dopamine norepinephrine epinephrine β- hydroxylase N-methyltransferase II. The adrenergic neuron A. neurotransmission at adrenergic neurons:

2.storage of norepinephrineinvesicles:Most of norepinephrine is packaged in vesicles3.releaseofnorepinephrine:an action potential reaches at the nerve ending,calciumchannels open, causing an increase in the concentration ofintracellular calcium.Elevated calcium levels promote the
2.storage of norepinephrine in vesicles: Most of norepinephrine is packaged in vesicles 3.release of norepinephrine : an action potential reaches at the nerve ending, calcium channels open, causing an increase in the concentration of intracellular calcium. Elevated calcium levels promote the

fusion of synaptic vesicles with the presynapticmembrane and release of NA or AD into thesynapticcleft.4.Bindingtoreceptor:norepinephrine may bind to and activate anadrenergic receptor
fusion of synaptic vesicles with the presynaptic membrane and release of NA or AD into the synaptic cleft. 4.Binding to receptor: norepinephrine may bind to and activate an adrenergic receptor

5.Degradationof norepinephrine:Uptake l: reuptake into the nerve terminalsThefate of recaptured norepinephrine.i:most of them into the storage vesiclesii: these who don't into vesicles can be oxidized bymonoamineoxidase(MAO)Uptake 2:into cardiac muscle or smooth musclecells Can be metabolized by COMT and MAO
Uptake 1: reuptake into the nerve terminals The fate of recaptured norepinephrine: i: most of them into the storage vesicles ii: these who don’t into vesicles can be oxidized by monoamine oxidase(MAO). Uptake 2: into cardiac muscle or smooth muscle cells Can be metabolized by COMT and MAO. 5.Degradation of norepinephrine :

A few diffuse out of synaptic space and enterthegeneralcirculation.Cotransmitters in Cholinergic and AdrenergicNerves This phenomenon that the vesicles of bothcholinergicandadrenergicnervescontainothersubstances in addition to the primary transmitter iscalledcotransport
A few diffuse out of synaptic space and enter the general circulation. Cotransmitters in Cholinergic and Adrenergic Nerves This phenomenon that the vesicles of both cholinergic and adrenergic nerves contain other substances in addition to the primary transmitter is called cotransport

PresynapticneuronendingActionTyrosinepotentialsCa+++DopaInactivatedDopaminebyMAONorepinephrineReuptake(most)CirculationCPNorepinephrineCCOReceptorInactivatedPostsynapticbyCOMTcellInactiveproducts儿茶酚胺的产生、释放及再摄取
儿茶酚胺的产生、释放及再摄取

SYMPATHETICNERVEVARICOSITYTYROSINEEFFECTORACELLNEPFTYROSINE1esOnse?NEBDOPAPNEG¥OR.RNEEDACDCOMTNENENMNvesiclesresponseENE工心NEMBRNENEURONEMAOEFFECTORJUNCTIONThe synthesis,release,reuptake,andmetabolism of Norepinephrine
The synthesis, release, reuptake, and metabolism of Norepinephrine

B.ADRENGICRECEPTORSa-adrenoceptor:a,anda,receptorsadrenoceptorsβ-adrenoceptor:B,,B, andB,receptors
B. ADRENGIC RECEPTORS adrenoceptors α-adrenoceptor: α1 andα2 receptors ß –adrenoceptor: ß1 , ß2 and ß3 receptors
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