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一种新型抗心律失常药物:Craviten(M - 71)对体外培养的心肌切片中三磷酸腺苷(ATP)水平的影响。

The effect of a new antiarrhythmic drug: Craviten (M-71) on the ATP level in heart muscle slices in vitro.

作者信息

Gumińska M, Kedryna T, Marchut E, Eckstein M

出版信息

Pol J Pharmacol Pharm. 1980 Nov-Dec;32(6):877-82.

PMID:7243683
Abstract

Under anaerobic conditions, in which glucose is the only energy source, the ATP level in heart muscle slices diminishes to about 50% of the control value during 60 min of incubation. The presence of a new antiarrhythmic drug, Craviten (Polfa) (2S, 2'S) N, N'-dimethyl-N, N'-bis-[1(3', 4', 5'-trimethoxybenzoyloxy)-butyl-2]-ethylenediamine dihydrochloride, (M-71), and to some extent also its 2R, 2'R isomer in 10 times greater concentration protects against this spontaneous ATP fall observed anaerobically in the control experiments. Under aerobic conditions, with glucose or palmitate as energy sources, Craviten even raises the ATP level in comparison to the initial control values. This effect is stereospecific, since the 2R, 2'R isomer does not change the aerobic ATP level, Quinidine and procaine amide used for comparison as standard antiarrhythmic drugs do not counteract the anaerobic ATP decrease, and under aerobic conditions they even enhance the ATP fall. Craviten, a new antiarrhythmic drug, exerts some stereospecific effect on energy metabolism and the ATP content in heart muscle slices in vitro.

摘要

在无氧条件下,葡萄糖是唯一的能量来源,心肌切片在孵育60分钟期间,其ATP水平降至对照值的约50%。一种新型抗心律失常药物Craviten(Polfa)(2S,2'S)N,N'-二甲基-N,N'-双-[1(3',4',5'-三甲氧基苯甲酰氧基)-丁基-2]-乙二胺二盐酸盐(M-71),以及在某种程度上其浓度高10倍的2R,2'R异构体,可防止在对照实验中观察到的无氧条件下ATP的自发下降。在有氧条件下,以葡萄糖或棕榈酸酯作为能量来源,与初始对照值相比,Craviten甚至能提高ATP水平。这种效应具有立体特异性,因为2R,2'R异构体不会改变有氧条件下的ATP水平。作为标准抗心律失常药物用于比较的奎尼丁和普鲁卡因酰胺不会抵消无氧条件下ATP的降低,并且在有氧条件下它们甚至会加剧ATP的下降。新型抗心律失常药物Craviten对体外心肌切片的能量代谢和ATP含量具有一些立体特异性作用。

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