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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。

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