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长期给予(-)司来吉兰(丙炔苯丙胺),一种可增强脑内多巴胺能张力的化合物,多巴胺受体对阿扑吗啡的敏感性保持不变。

Long-term administration of (-)deprenyl (selegiline), a compound which facilitates dopaminergic tone in the brain, leaves the sensitivity of dopamine receptors to apomorphine unchanged.

作者信息

Timar J, Knoll B, Knoll J

出版信息

Arch Int Pharmacodyn Ther. 1986 Dec;284(2):255-66.

PMID:3103558
Abstract

The effect of repeated administration of the MAO-B enzyme blocker (-)deprenyl on the apomorphine (APO) sensitivity of dopamine (DA) receptors was investigated in rats, and compared to the effect of other drugs influencing the dopaminergic system. APO was given either in a high dose (0.1-0.6 mg/kg), which induces stereotyped behaviour or in a smaller one (0.02 mg/kg) causing sedation. Repeated administration of all the other drugs investigated (except (-)deprenyl), i.e. haloperidol, d-amphetamine, (1 mg/kg s.c., respectively) and the MAO-A blocker clorgyline (0.25 mg/kg s.c.) altered the efficiency of APO on the stereotypy. Haloperidol, clorgyline (0.5 mg/kg s.c.) and imipramine (10 mg/kg i.p.) attenuated the APO-sedation. The long-lasting administration of (-)deprenyl (0.25 mg/kg s.c., daily for 42 days) however, left the effects of APO unchanged, demonstrating that (-)deprenyl facilitates the dopaminergic tone in the rat brain without altering the sensitivity of DA receptors.

摘要

在大鼠中研究了重复给予单胺氧化酶B(MAO-B)酶阻断剂(-)司来吉兰对多巴胺(DA)受体阿扑吗啡(APO)敏感性的影响,并与其他影响多巴胺能系统的药物的作用进行了比较。给予高剂量(0.1 - 0.6mg/kg)的APO可诱导刻板行为,给予较小剂量(0.02mg/kg)则引起镇静。重复给予所有其他研究的药物(除了(-)司来吉兰),即氟哌啶醇、右旋苯丙胺(分别为1mg/kg皮下注射)和单胺氧化酶A(MAO-A)阻断剂氯吉兰(0.25mg/kg皮下注射),均改变了APO对刻板行为的作用效率。氟哌啶醇、氯吉兰(0.5mg/kg皮下注射)和丙咪嗪(10mg/kg腹腔注射)减弱了APO诱导的镇静作用。然而,长期给予(-)司来吉兰(0.25mg/kg皮下注射,每日一次,共42天),APO的作用未发生改变,表明(-)司来吉兰可增强大鼠脑内的多巴胺能张力,而不改变DA受体的敏感性。

相似文献

1
Long-term administration of (-)deprenyl (selegiline), a compound which facilitates dopaminergic tone in the brain, leaves the sensitivity of dopamine receptors to apomorphine unchanged.长期给予(-)司来吉兰(丙炔苯丙胺),一种可增强脑内多巴胺能张力的化合物,多巴胺受体对阿扑吗啡的敏感性保持不变。
Arch Int Pharmacodyn Ther. 1986 Dec;284(2):255-66.
2
The effect of (-) deprenyl (selegiline) on different behavioral changes induced by dopamine agonists in the rat.(-)去甲丙咪嗪(司来吉兰)对多巴胺激动剂诱导的大鼠不同行为变化的影响。
Pol J Pharmacol Pharm. 1988 Nov-Dec;40(6):659-66.
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The effect of repeated administration of (-) deprenyl on the phenylethylamine-induced stereotypy in rats.重复给予(-)司来吉兰对大鼠苯乙胺诱导的刻板行为的影响。
Arch Int Pharmacodyn Ther. 1986 Jan;279(1):50-60.
4
The effect of repeated doses of (-) deprenyl on the dynamics of monoaminergic transmission. Comparison with clorgyline.重复剂量的(-)司来吉兰对单胺能传递动力学的影响。与氯吉兰的比较。
Pol J Pharmacol Pharm. 1986 Jan-Feb;38(1):57-67.
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R-(-)-deprenyl (Selegiline, Movergan) facilitates the activity of the nigrostriatal dopaminergic neuron.R-(-)-司来吉兰(Selegiline,Movergan)可促进黑质纹状体多巴胺能神经元的活性。
J Neural Transm Suppl. 1987;25:45-66.
6
Inhibition of monoamine oxidase-B by (-)-deprenyl potentiates neuronal responses to dopamine agonists but does not inhibit dopamine catabolism in the rat striatum.(-)-司来吉兰对单胺氧化酶-B的抑制作用增强了大鼠纹状体中神经元对多巴胺激动剂的反应,但并不抑制多巴胺的分解代谢。
J Pharmacol Exp Ther. 1991 Sep;258(3):1019-26.
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Behavioral effects of deprenyl in aged rats.
Funct Neurol. 1986 Apr-Jun;1(2):165-74.
8
Recovery of MAO-B enzyme activity after (-)deprenyl (selegiline) pretreatment, measured in vivo.体内测量(-)司来吉兰(司来吉兰)预处理后MAO-B酶活性的恢复情况。
Acta Physiol Hung. 1989;74(3-4):259-66.
9
Injection of apomorphine--a test to predict individual different dopaminergic sensitivity?注射阿扑吗啡——一种预测个体不同多巴胺能敏感性的测试?
J Neural Transm Suppl. 1995;45:143-55.
10
Repeated administration of (-)deprenyl leaves the mesolimbic dopaminergic activity unchanged.重复给予(-)司来吉兰不会改变中脑边缘多巴胺能活性。
Acta Physiol Hung. 1990;75 Suppl:133-4.

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