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尼麦角林对各种形式环磷酸腺苷磷酸二酯酶反应动力学的影响。

The influence of nicergoline on reaction kinetics of various forms of cyclic AMP phosphodiesterase.

作者信息

Pericin D, Leskovac V

出版信息

Arzneimittelforschung. 1981;31(12):2082-5.

PMID:6277342
Abstract

10-Methoxy-1,6-dimethylergoline-8 beta-methanol-5-bromonicotinate (nicergoline) has in vitro a modulatory effect upon reaction kinetics of various forms of cAMP phosphodiesterase (PDE) from beef heart and mice brain. Nicergoline inhibits low Km form of cAMP PDE from hear and brain; concentration of inhibitor required for 50% inhibition is 3-12 mumol/l. It is believe that the observed in vitro effects of nicergoline on reaction kinetics of various forms of cAMP PDE may in vivo help to normalize the level of cAMP, keep its concentration within certain limits, both by opposing large increase and large decrease in its cellular concentration.

摘要

10-甲氧基-1,6-二甲基麦角灵-8β-甲醇-5-溴烟酸酯(尼麦角林)在体外对来自牛心和小鼠脑的各种形式的环磷酸腺苷磷酸二酯酶(PDE)的反应动力学具有调节作用。尼麦角林抑制心脏和脑中低Km形式的环磷酸腺苷磷酸二酯酶;50%抑制所需的抑制剂浓度为3-12μmol/L。据信,尼麦角林在体外对各种形式的环磷酸腺苷磷酸二酯酶反应动力学的作用,在体内可能有助于使环磷酸腺苷水平正常化,通过对抗其细胞内浓度的大幅升高和大幅降低,将其浓度保持在一定范围内。

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