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长期使用纳曲酮可抑制既往海洛因成瘾者体内由肾上腺素和5-羟色胺诱导的血小板聚集。

Chronic naltrexone suppresses platelet aggregation induced by adrenaline and 5-hydroxytryptamine in former heroin addicts.

作者信息

García-Sevilla J A, Ulibarri I, Giralt M T, Areso P, Oliveros R G, Gutiérrez M

机构信息

Department of Pharmacology, Faculty of Medicine, University of the Basque Country, Leioa.

出版信息

J Neural Transm. 1988;73(2):157-60. doi: 10.1007/BF01243386.

DOI:10.1007/BF01243386
PMID:3210007
Abstract

Naltrexone, an opioid receptor antagonist, is used as an adjunct in the treatment of opiate addiction. In former heroin addicts, long-term treatment with naltrexone (350 mg/week for 5 months) resulted in suppression of adrenaline and 5-hydroxytryptamine (5-HT)-induced platelet aggregation. The results demonstrate that sustained blockade of opioid receptors can impair the functional expression of alpha 2-adrenoceptors and 5-HT2 receptors in human platelets. These findings may have negative clinical implications in the treatment of opiate addiction with naltrexone.

摘要

纳曲酮是一种阿片受体拮抗剂,用作治疗阿片成瘾的辅助药物。在既往海洛因成瘾者中,长期使用纳曲酮治疗(350毫克/周,持续5个月)导致肾上腺素和5-羟色胺(5-HT)诱导的血小板聚集受到抑制。结果表明,阿片受体的持续阻断会损害人血小板中α2-肾上腺素能受体和5-HT2受体的功能表达。这些发现可能对纳曲酮治疗阿片成瘾具有负面临床意义。

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1
Chronic naltrexone suppresses platelet aggregation induced by adrenaline and 5-hydroxytryptamine in former heroin addicts.长期使用纳曲酮可抑制既往海洛因成瘾者体内由肾上腺素和5-羟色胺诱导的血小板聚集。
J Neural Transm. 1988;73(2):157-60. doi: 10.1007/BF01243386.
2
Heroin increases the density and sensitivity of platelet alpha 2-adrenoceptors in human addicts.海洛因会增加人类成瘾者血小板α2肾上腺素能受体的密度和敏感性。
Psychopharmacology (Berl). 1986;88(4):489-92. doi: 10.1007/BF00178512.
3
Platelet alpha 2-adrenoceptors in heroin addicts during withdrawal and after treatment with clonidine.
Eur J Pharmacol. 1985 Aug 27;114(3):365-74. doi: 10.1016/0014-2999(85)90382-6.
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Cortisol levels during chronic naltrexone maintenance treatment in ex-opiate addicts.阿片类药物成瘾者在长期纳曲酮维持治疗期间的皮质醇水平。
Biol Psychiatry. 1986 Feb;21(2):217-20. doi: 10.1016/0006-3223(86)90150-2.
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Urapidil inhibits 5-hydroxytryptamine induced platelet aggregation and 14C-5-hydroxytryptamine uptake in platelets.乌拉地尔抑制5-羟色胺诱导的血小板聚集以及血小板对14C-5-羟色胺的摄取。
Curr Med Res Opin. 1990;12(2):86-92. doi: 10.1185/03007999009110475.
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Investigations on 5-HT₄ receptor expression and effects of tegaserod on human platelet aggregation in vitro.5-HT₄ 受体表达的研究及替加色罗对人血小板聚集的体外作用。
Am J Ther. 2010 Nov-Dec;17(6):543-52. doi: 10.1097/MJT.0b013e3181b63f21.
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Nontolerance to the opioid antagonism of naltrexone.
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Five-year follow-up of opiate addicts with naltrexone and behavior therapy.纳曲酮与行为疗法治疗阿片类成瘾者的五年随访
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Potentiation of ADP-induced aggregation in human platelet-rich plasma by 5-hydroxytryptamine and adrenaline.5-羟色胺和肾上腺素对人富血小板血浆中ADP诱导的聚集作用的增强
Br J Pharmacol. 1992 Aug;106(4):917-23. doi: 10.1111/j.1476-5381.1992.tb14435.x.
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Craving in heroin addicts maintained on the opiate antagonist naltrexone.对维持使用阿片类拮抗剂纳曲酮的海洛因成瘾者的渴望。
Am J Drug Alcohol Abuse. 1978;5(4):415-23. doi: 10.3109/00952997809007017.

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Characterization of the Presence and Function of Platelet Opioid Receptors.血小板阿片受体的存在及其功能的表征
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2
The Effect of Psychoactive Drugs on in vitro Platelet Function.精神活性药物对体外血小板功能的影响。
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本文引用的文献

1
Evidence for functional 5-HT2 receptor sites on human blood platelets.人体血小板上功能性5-羟色胺2受体位点的证据。
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Opiate receptors on lymphocytes and platelets in man.
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Naltrexone-induced opiate receptor supersensitivity.纳曲酮诱导的阿片受体超敏反应。
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Do human platelets have opiate receptors?人类血小板有阿片受体吗?
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Interaction of selective alpha-adrenoceptor agonists and antagonists with human and rabbit blood platelets.选择性α-肾上腺素能受体激动剂与拮抗剂与人及兔血小板的相互作用。
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6
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.
7
Heroin increases the density and sensitivity of platelet alpha 2-adrenoceptors in human addicts.海洛因会增加人类成瘾者血小板α2肾上腺素能受体的密度和敏感性。
Psychopharmacology (Berl). 1986;88(4):489-92. doi: 10.1007/BF00178512.
8
Opiate and alpha 2-adrenoceptor responses of rat amygdaloid neurons: co-localization and interactions during withdrawal.大鼠杏仁核神经元的阿片类和α2-肾上腺素能受体反应:戒断期间的共定位和相互作用
J Neurosci. 1985 Nov;5(11):3016-24. doi: 10.1523/JNEUROSCI.05-11-03016.1985.
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Increased analgesic potency of morphine and increased brain opioid binding sites in the rat following chronic naltrexone treatment.慢性纳曲酮治疗后大鼠吗啡镇痛效力增强及脑内阿片类结合位点增加。
Life Sci. 1985 Jun 17;36(24):2325-32. doi: 10.1016/0024-3205(85)90322-4.
10
Blockade of alpha 2-adrenoceptors permits the operation of otherwise silent opioid kappa-receptors at the sympathetic axons of rabbit jejunal arteries.α2 -肾上腺素能受体的阻断可使原本沉默的阿片κ受体在兔空肠动脉的交感神经轴突上发挥作用。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Sep;334(1):48-55. doi: 10.1007/BF00498739.