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青藤碱及其某些衍生物以及它们与左旋多巴联合使用对生物源性单胺类物质脑内水平的影响。

Effects of glaucine and some glaucine derivatives and of their combination with L-DOPA on the brain level of biogenic monoamines.

作者信息

Petkov V, Yanev S, Stancheva S

出版信息

Arch Int Pharmacodyn Ther. 1982 Sep;259(1):83-92.

PMID:7181577
Abstract

Glaucine and two of its structural analogues exerted an inhibitory effect on phosphodiesterase activity in different tissue homogenates. In experiments on rats glaucine applied intraperitoneally significantly increased the brain level of dopamine (DA) and did not change the content of noradrenaline and serotonin (5-HT). The combined application of L-DOPA and glaucine or glaucine derivatives produced a higher increase in brain DA than the increase which would be expected by simple summation of the effects of L-DOPA and glaucine and of the glaucine derivatives respectively. At the same time L-DOPA and glaucine, applied together, caused a slighter decrease of brain 5-HT than the decrease produced by the same dose of L-DOPA when the latter was applied alone. It is suggested that the higher increase of brain DA produced by the combination of L-DOPA and the phosphodiesterase inhibitor glaucine or its structural analogues is mainly due to the increased cAMP level.

摘要

青藤碱及其两种结构类似物对不同组织匀浆中的磷酸二酯酶活性具有抑制作用。在对大鼠进行的实验中,腹腔注射青藤碱可显著提高大脑中多巴胺(DA)的水平,而不改变去甲肾上腺素和5-羟色胺(5-HT)的含量。左旋多巴(L-DOPA)与青藤碱或青藤碱衍生物联合应用时,大脑中DA的增加量高于分别简单相加L-DOPA与青藤碱以及青藤碱衍生物的作用所预期的增加量。同时,L-DOPA与青藤碱联合应用时,大脑5-HT的降低程度比单独应用相同剂量的L-DOPA时要小。提示L-DOPA与磷酸二酯酶抑制剂青藤碱或其结构类似物联合应用导致大脑DA升高幅度更大,主要是由于环磷酸腺苷(cAMP)水平升高所致。

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