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戒断期海洛因成瘾者中α2-肾上腺素能受体介导的血小板腺苷酸环化酶活性抑制

Alpha 2-adrenoceptor-mediated inhibition of platelet adenylate cyclase activity in heroin addicts in abstinence.

作者信息

García-Sevilla J A, Ulibarri I, Ugedo L, Gutierrez M

出版信息

Psychopharmacology (Berl). 1987;92(3):320-3. doi: 10.1007/BF00210837.

DOI:10.1007/BF00210837
PMID:2819917
Abstract

The inhibition of basal and forskolin-stimulated platelet adenylate cyclase activity by (-)adrenaline was studied in ten heroin addicts during spontaneous withdrawal. Both basal and forskolin-stimulated enzyme activities were increased during heroin withdrawal and the inhibitory effect induced by (-)adrenaline was potentiated with parallel shifts to the left of the concentration-effect curves. The number of binding sites for 3Hadrenaline in platelet membranes was also increased during withdrawal. Treatment with clonidine markedly attenuated the inhibitory effect induced by (-)adrenaline on platelet adenylate cyclase activity. The results indicate that the heroin withdrawal syndrome induces supersensitivity of the platelet alpha 2-adrenoceptor-adenylate cyclase system.

摘要

在十名海洛因成瘾者自然戒断期间,研究了(-)肾上腺素对基础状态及福斯高林刺激的血小板腺苷酸环化酶活性的抑制作用。在海洛因戒断期间,基础及福斯高林刺激的酶活性均升高,且(-)肾上腺素诱导的抑制作用增强,浓度-效应曲线平行左移。戒断期间血小板膜上[3H](-)肾上腺素的结合位点数量也增加。可乐定治疗显著减弱了(-)肾上腺素对血小板腺苷酸环化酶活性的抑制作用。结果表明,海洛因戒断综合征诱导血小板α2-肾上腺素能受体-腺苷酸环化酶系统超敏。

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1
Alpha 2-adrenoceptor-mediated inhibition of platelet adenylate cyclase activity in heroin addicts in abstinence.戒断期海洛因成瘾者中α2-肾上腺素能受体介导的血小板腺苷酸环化酶活性抑制
Psychopharmacology (Berl). 1987;92(3):320-3. doi: 10.1007/BF00210837.
2
Platelet alpha 2-adrenoceptors in heroin addicts during withdrawal and after treatment with clonidine.
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Alpha 2-adrenoceptor coupling to adenylate cyclase in adrenaline insensitive human platelets.
Eur J Pharmacol. 1985 Oct 8;116(1-2):113-9. doi: 10.1016/0014-2999(85)90191-8.
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The local anaesthetic benzyl alcohol attenuates the alpha 2-adrenoceptor-mediated inhibition of human platelet adenylate cyclase activity when stimulated by prostaglandin E1, but not that stimulated by forskolin.当受到前列腺素E1刺激时,局部麻醉剂苯甲醇会减弱α2-肾上腺素能受体介导的对人血小板腺苷酸环化酶活性的抑制作用,但对受福斯高林刺激时的抑制作用则无此影响。
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Uncoupling of the platelet alpha 2-adrenoceptor adenylate cyclase system by N-ethylmaleimide and the resulting effect on receptor density and sensitivity.N-乙基马来酰亚胺对血小板α2-肾上腺素能受体腺苷酸环化酶系统的解偶联作用及其对受体密度和敏感性的影响。
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Eur J Pharmacol. 1984 Apr 13;100(1):131-2. doi: 10.1016/0014-2999(84)90327-3.
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Species differences in alpha 2-adrenergic regulation of platelet adenylate cyclase.α2-肾上腺素能对血小板腺苷酸环化酶调节的种属差异
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Uncoupling of alpha-adrenoceptor-mediated inhibition of human platelet adenylate cyclase by N-ethylmaleimide.N-乙基马来酰亚胺对α-肾上腺素能受体介导的人血小板腺苷酸环化酶抑制作用的解偶联
J Biol Chem. 1982 Mar 25;257(6):2829-33.

引用本文的文献

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mu-Opioid receptor and alpha 2-adrenoceptor agonist binding sites in the postmortem brain of heroin addicts.海洛因成瘾者死后大脑中的μ-阿片受体和α2-肾上腺素能受体激动剂结合位点
Psychopharmacology (Berl). 1994 Jun;115(1-2):135-40. doi: 10.1007/BF02244763.
2
Modulation of brain alpha 2-adrenoceptor and mu-opioid receptor densities during morphine dependence and spontaneous withdrawal in rats.大鼠吗啡依赖及自然戒断过程中脑α2-肾上腺素能受体和μ-阿片受体密度的调节
Naunyn Schmiedebergs Arch Pharmacol. 1987 Nov;336(5):530-7. doi: 10.1007/BF00169310.

本文引用的文献

1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Forskolin, adenylate cyclase, and cell physiology: an overview.福斯高林、腺苷酸环化酶与细胞生理学:综述
Adv Cyclic Nucleotide Protein Phosphorylation Res. 1984;17:81-9.
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Interaction of forskolin with resolved adenylate cyclase components.福斯高林与解离的腺苷酸环化酶组分的相互作用。
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Opiate receptors on lymphocytes and platelets in man.
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Alpha 2-adrenoreceptors on human platelets: selective labelling by [3H]clonidine and [3H]yohimbine and competitive inhibition by antidepressant drugs.人血小板上的α2-肾上腺素能受体:[3H]可乐定和[3H]育亨宾的选择性标记以及抗抑郁药物的竞争性抑制作用
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Effect of acute methadone withdrawal on prostaglandin E-stimulated 3H-cyclic adenosine monophosphate accumulation in human platelets.
Clin Pharmacol Ther. 1980 May;27(5):607-11. doi: 10.1038/clpt.1980.86.
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Effects of alpha 2-adrenoceptor agonists and of related compounds on aggregation of, and on adenylate cyclase activity in, human platelets.α2 -肾上腺素能受体激动剂及相关化合物对人血小板聚集和腺苷酸环化酶活性的影响。
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A highly sensitive adenylate cyclase assay.一种高灵敏度的腺苷酸环化酶检测方法。
Anal Biochem. 1974 Apr;58(2):541-8. doi: 10.1016/0003-2697(74)90222-x.
9
Activation of presynaptic alpha 2-adrenoceptors attenuates the inhibitory effect of mu-opioid receptor agonists on noradrenaline release from brain slices.突触前α2肾上腺素能受体的激活减弱了μ阿片受体激动剂对脑片去甲肾上腺素释放的抑制作用。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Aug;333(4):377-80. doi: 10.1007/BF00500012.
10
Labelling of human platelet alpha 2-adrenoceptors with the full agonist [3H](-)adrenaline.用完全激动剂[³H](-)肾上腺素标记人血小板α₂-肾上腺素能受体。
Eur J Pharmacol. 1986 May 13;124(1-2):31-41. doi: 10.1016/0014-2999(86)90121-4.