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(-)司来吉兰代谢为苯丙胺和甲基苯丙胺可能是其治疗益处的原因:一项生化评估。

Metabolism of (-) deprenyl to amphetamine and methamphetamine may be responsible for deprenyl's therapeutic benefit: a biochemical assessment.

作者信息

Karoum F, Chuang L W, Eisler T, Calne D B, Liebowitz M R, Quitkin F M, Klein D F, Wyatt R J

出版信息

Neurology. 1982 May;32(5):503-9. doi: 10.1212/wnl.32.5.503.

DOI:10.1212/wnl.32.5.503
PMID:6803190
Abstract

The urinary excretion of some important phenylethylamines, catecholamines, their metabolites, amphetamine, and methamphetamine were measured in parkinsonian patients on Sinemet (L-dopa plus carbidopa, a peripheral dopadecarboxylase inhibitor) and depressed patients after chronic (-) deprenyl treatment. Deprenyl was efficiently metabolized to amphetamine and methamphetamine. It increased the excretion of phenylethylamine and of m- and p-tyramine, and reduced the output of norepinephrine metabolites, but failed to alter the excretion of dopamine-deaminated metabolites. These changes were attributed more to amphetamine and methamphetamine than to inhibition of monoamine oxidase type B. Sinemet treatment alone increased the excretion of dopamine, 3-methoxytyramine, and their respective deaminated metabolites, 3, 4-dihydroxyphenylacetic acid and homovanillic acid. It is concluded that conversion of deprenyl to amphetamine and methamphetamine may contribute to some of the therapeutic benefits of deprenyl.

摘要

对服用息宁(左旋多巴加卡比多巴,一种外周多巴脱羧酶抑制剂)的帕金森病患者以及接受慢性(-)司来吉兰治疗后的抑郁症患者,测定了一些重要的苯乙胺、儿茶酚胺、它们的代谢产物、苯丙胺和甲基苯丙胺的尿排泄量。司来吉兰能有效地代谢为苯丙胺和甲基苯丙胺。它增加了苯乙胺以及间酪氨酸和对酪氨酸的排泄量,并减少了去甲肾上腺素代谢产物的排出量,但未能改变多巴胺脱氨基代谢产物的排泄量。这些变化更多地归因于苯丙胺和甲基苯丙胺,而非对B型单胺氧化酶的抑制作用。单独使用息宁治疗会增加多巴胺、3-甲氧基酪胺及其各自的脱氨基代谢产物3,4-二羟基苯乙酸和高香草酸的排泄量。得出的结论是,司来吉兰转化为苯丙胺和甲基苯丙胺可能有助于司来吉兰的一些治疗益处。

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