(-)去戊烯醇(Selegiline):过去、现在和未来。

Neurobiology (Budapest, Hungary) Pub Date : 2000-01-01
J Knoll
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引用次数: 0

摘要

(-)去戊烯酰(Selegiline)是(-)甲基苯丙胺的n -丙炔类似物,是临床病例中唯一一种通过增强冲动传播介导的脑内去甲肾上腺素和多巴胺的释放(儿茶酚胺能活性增强剂,CAE,效应),使儿茶酚胺能脑系统在小剂量无副作用的情况下保持较高活性水平的药物。(-)去戊烯醇选择性地刺激大脑中的儿茶酚胺能神经元,因为与PEA和苯丙胺不同,它们会诱导去甲肾上腺素和多巴胺从神经元内持续释放,(-)去戊烯醇没有这种特性。由于CAE的作用,a)大鼠在发育后阶段维持去戊烯醇(-),可以减缓与年龄相关的性和学习能力下降,显著延长寿命;b)早期、未经治疗的帕金森病患者持续服用去丙烯醇(-)的时间明显晚于对照组,且左旋多巴加去丙烯醇(-)的寿命明显长于单独服用左旋多巴的患者;c)在中度重度阿尔茨海默病患者中,用(-)去戊烯醇治疗可以减缓疾病的进展。我们有理由认为,在发育后阶段预防性低剂量使用安全的儿茶酚胺能活性增强物质将减缓与年龄相关的行为表现下降,延缓自然死亡,降低对帕金森病和阿尔茨海默病的易感性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
(-)Deprenyl (Selegiline): past, present and future.

(-)Deprenyl (Selegiline), the N-propargyl analogue of (-)methamphetamine, is the only drug in clinical case which, by enhancing the impulse propagation mediated release of noradrenaline and dopamine in the brain (catecholaminergic activity enhancer, CAE, effect), keeps in small doses without side-effects the catecholaminergic brain system on a higher activity level. (-)Deprenyl stimulates the catecholaminergic neurons selectively in the brain because, in contrast to PEA and the amphetamines which induce the continuous release of noradrenaline and dopamine from their intraneuronal stores, (-)deprenyl is devoid of this property. It is due to the CAE effect that a) the maintenance of rats on (-)deprenyl during the postdevelopmental phase of their life slows the age-related decline of sexual and learning performances and prolongs life significantly; b) patients with early, untreated Parkinson's disease maintained on (-)deprenyl need levodopa significantly later than their placebo-treated peers, and when on levodopa plus (-)deprenyl, they live significantly longer than patients on levodopa alone; and c) in patients with moderately severe impairment from Alzheimer's disease, treatment with (-)deprenyl slows the progression of the disease. It is reasonable to expect that a prophylactic low dose administration of a safe catecholaminergic activity enhancer substance during the postdevelopmental phase of life will slow the age-related decline of behavioral performances, delay natural death and decrease susceptibility to Parkinson's disease and Alzheimer's disease.

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