(二) α-、β-受体激动剂1.肾上腺素Epinephrine.PPTVIP

(二) α-、β-受体激动剂1.肾上腺素Epinephrine.PPT

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(二) α-、β-受体激动剂1.肾上腺素Epinephrine.PPT

Epinephrine or adrenaline Norepinephrine or noradrenaline belong to Catecholamines 邻苯二酚,儿茶酚:Catechol The biosynthesis and metabolism of noradrenaline (1) L-tyrosine dopa dopamine The biosynthesis and metabolism of noradrenaline (2) MAO(Monoamine oxidase) COMT(Catechol-O-methyltransferase) AR(aldehyde reductase ) AD (aldehyde dehydrogenase) 7.2 Adrenergic drugs 1. α-receptor or α-, β-receptor agonists (1) α-receptor agonists Norepinephrine Bitartrate R-(-)-4-(2-氨基-1-羟基乙基)-1,2-苯二酚 R,R-2,3-二羟基丁二酸盐一水合物 R-(-)-4-(2-Amino-1-hydroxyethyl)-1,2-benzenediol R,R-2,3-dihydroxy-butanedionate (1:1) salt monohydrate activity of (-)-body is 27 times than (+)-body. heat for 3 minutes at 120 ℃ or heat with concentrated sulfuric acid at 80 ~ 90 ℃ for 2 hours, racemization will be occurred; norepinephrine is easily oxidized under light or air, so it should be preserved without contacting with air. norepinephrine will be oxidized into norepinephrine red in the buffer solution of pH 6.5 added with iodine solution, sodium thiosulfate can fade the colour of iodine solution and then change into red. (二) α-、β-受体激动剂 1.肾上腺素 Epinephrine R-4-[(甲胺基)-1-羟基乙基]-1,2苯二酚 Although there is no oral adrenergic activity, the clinical use is much borader than norepinephrine. α-receptor agonist, contract blood vessels, increase blood pressure.For emergency treatment of anaphylactic shock; β1-receptor agonist, excite cardiac muscle. treatment of cardiac arrest; β2- receptor agonist, relax bronchia. Remission of asthma 2.麻黄碱 Ephedrine Ephedrine is seperated from several Ephedra plants. in 1887, isolated from the Chinese herb Ephedra and pure Ephedrine was crystallized. Its clinical application was earlier than norepinephrine and epinephrine (-)ephedrine* (-)pseudo~ (+)ephedrine (+)pseudo~ (1R,2S) (1R,2R) (1S,2R) (1S,2S) 化学结构: 1. 与肾上腺素相比,增加CH3,没有3,4-二羟基 2. 有2个手性C,4个异构体 用途:与肾上腺素相似,支气管舒张;血管升压;心脏兴奋剂;鼻充血治疗药

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