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[新合成的1,3 - 二甲基黄嘌呤衍生物对各种组织匀浆中3',5'-环磷酸腺苷磷酸二酯酶活性的抑制作用]

[Inhibitory action of newly synthesized 1,3-dimethylxanthine derivatives on the 3',5'-cyclic AMP phosphodiesterase activity of the homogenates of various tissues].

作者信息

Staneva D, Bogoslovova T, Pankova A

出版信息

Eksp Med Morfol. 1980;19(3):154-9.

PMID:6252004
Abstract

The authors examined the action of fine newly synthesized xanthine derivatives on the activity of the enzyme 3',5' AMP phosphodiesterase (at high substrate concentrations) in homogenates, obtained from the brain lung and myocardium of a rat. The compounds were compared with theophylline for their activity. They showed low inhibiting activity in brain homogenates in contrast to the manifested activity of some of them in lungs and myocardium. Especially manifested difference was observed for the compound with a code 1t which was find times stronger inhibitor in the lung than in the brain. The authors make an inference that some of the compounds manifect selective activity as inhibitors of the enzyme phosphodiesterase and in this sense the search for xanthine derivatives with specific activity is prespective.

摘要

作者研究了新合成的精细黄嘌呤衍生物对大鼠脑、肺和心肌匀浆中3',5'-AMP磷酸二酯酶(在高底物浓度下)活性的作用。将这些化合物与茶碱的活性进行了比较。与它们在肺和心肌中表现出的活性相反,它们在脑匀浆中显示出低抑制活性。对于编号为1t的化合物,观察到特别明显的差异,该化合物在肺中作为抑制剂的活性比在脑中强5倍。作者推断,一些化合物表现出作为磷酸二酯酶抑制剂的选择性活性,从这个意义上说,寻找具有特定活性的黄嘌呤衍生物是有前景的。

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