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[3-乙氧羰基氨基-5-二甲基氨基乙酰亚氨基二苄基盐酸盐(邦尼可,AWD 19-166,GS 015)的抗心律失常作用特征]

[Characteristics of the anti-arrhythmic action of 3-carbethoxyamino-5-dimethylaminoacetyl-imino-dibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015)].

作者信息

Kaverina N V, Berdjajev S J, Darinskij N V

出版信息

Pharmazie. 1985 Dec;40(12):840-4.

PMID:3841598
Abstract

The action of GS 015, a substance out of the series of the novel 5-(dialkyl-amino-acyl)-3-carbalkoxyamino-10,11-dihydro-5H-dibenz[b ,f]azepines, on the alteration of the bioelectric activity in the sympathetic nerves of the heart in case of disturbed cardiac rhythm and ventricular fibrillation was tested on anaesthetized cats. The arrhythmias were induced by two different methods: Artificial electric induction by high-frequency electrical stimulation of the ventricles, occlusion and reperfusion of the anterior descending branch of the arteria coronaria sinistra. GS 015 decreases the tonic bioelectric activity in the sympathetic nerves of the heart and prevents their activation in case of disturbed rhythm which is provoked or by electric stimulation or by occlusion of the coronary artery. With an electric stimulation of the ventricles GS 015, given at doses of 0.5, 1.0, and 2.0 mg/kg, decreases the maximally reproducible frequency in dependence on the dose, which corresponds to an increase of the effective refractory period. At the same time the fibrillation threshold of the ventricles is enhanced in a very intense and long-lasting manner excelling considerably the action of the reference preparations Ethmozin and lidocaine. It may be concluded from the present results that the antiarrhythmic and antifibrillatory effects of GS 015 are basing not only on its immediate action on the myocardial cell but also on a decrease of the activity in the sympathetic nerves of the heart.

摘要

在麻醉猫身上测试了新型5 -(二烷基氨基酰基)- 3 - 烷氧羰基氨基 - 10,11 - 二氢 - 5H - 二苯并[b,f]氮杂䓬系列中的一种物质GS 015对心律失常和心室颤动时心脏交感神经生物电活动改变的作用。心律失常通过两种不同方法诱发:通过高频电刺激心室进行人工电诱导,以及左冠状动脉前降支的闭塞和再灌注。GS 015降低心脏交感神经的紧张性生物电活动,并在由电刺激或冠状动脉闭塞引发的节律紊乱情况下防止其激活。在心室电刺激时,以0.5、1.0和2.0mg/kg的剂量给予GS 015,可根据剂量降低最大可重复频率,这对应于有效不应期的延长。同时,心室的颤动阈值以非常强烈和持久的方式提高,大大超过参比制剂乙吗噻嗪和利多卡因的作用。从目前的结果可以得出结论,GS 015的抗心律失常和抗纤颤作用不仅基于其对心肌细胞的直接作用,还基于心脏交感神经活动的降低。

相似文献

1
[Characteristics of the anti-arrhythmic action of 3-carbethoxyamino-5-dimethylaminoacetyl-imino-dibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015)].[3-乙氧羰基氨基-5-二甲基氨基乙酰亚氨基二苄基盐酸盐(邦尼可,AWD 19-166,GS 015)的抗心律失常作用特征]
Pharmazie. 1985 Dec;40(12):840-4.
2
[Circulatory action and adverse effects of 3-carbethoxyamino-5-dimethylamino-acetyl-iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015) in the dog and cat].[3-乙氧羰基氨基-5-二甲基氨基-乙酰亚氨基二苄基盐酸盐(邦尼可,AWD 19 - 166,GS 015)对犬猫的循环作用及不良反应]
Pharmazie. 1985 Dec;40(12):857-61.
3
[Antiarrhythmic effectiveness of 3-carbalkoxyamino-5-(omega-aminoacyl)-10,11-dihydro-5H-dibenz-[b,f]- azepines].[3-烷氧羰基氨基-5-(ω-氨基酰基)-10,11-二氢-5H-二苯并[b,f]氮杂卓的抗心律失常作用]
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[Antifibrillatory and anti-arrhythmic action of 3-carbethoxyamino-5-dimethylamino-acetyl iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015) on models of myocardial ischemia].[3-乙氧羰基氨基-5-二甲氨基-乙酰亚氨基二苄基盐酸盐(邦尼可,AWD 19 - 166,GS 015)对心肌缺血模型的抗纤颤和抗心律失常作用]
Pharmazie. 1985 Dec;40(12):845-7.
5
[Antiarrhythmic action of 3-carbethoxyamino-5-dimethylaminoacetyl-iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS -15) on experimental arrhythmia induced by aconitin, ouabain, calcium chloride and barium chloride].[盐酸3-乙氧羰基氨基-5-二甲氨基乙酰亚氨基二苄(邦尼可,AWD 19-166,GS-15)对乌头碱、哇巴因、氯化钙和氯化钡诱发的实验性心律失常的抗心律失常作用]
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[Clinico-electrophysiologic studies on the action of the anti-arrhythmic substance 3-carbethoxyamino-5-dimethylamino-acetyl-10,11-dihydro-5H- dibenz[b,f]azepine hydrochloride (Bonnecor, AWD 19-166, GS 015)].[抗心律失常药物盐酸3-乙氧羰基氨基-5-二甲氨基-乙酰基-10,11-二氢-5H-二苯并[b,f]氮杂卓(邦尼可,AWD 19-166,GS 015)作用的临床电生理研究]
Pharmazie. 1985 Dec;40(12):862-4.
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[New derivatives of 10,11-dihydro-5H-dibenz[b,f]azepine with antiarrhythmic action].具有抗心律失常作用的10,11-二氢-5H-二苯并[b,f]氮杂䓬新衍生物
Pharmazie. 1985 Dec;40(12):827-30.
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[Pharmacokinetics and pharmacodynamics of 3-carbethoxyamino-5-dimethylamino-acetyl-iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015) in the dog].
Pharmazie. 1985 Dec;40(12):869-70.
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[Pharmacokinetics and pharmacodynamics of 3-carbethoxyamino-5-dimethylamino-acetyl-iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS 015) in the cat].3-乙氧羰基氨基-5-二甲氨基-乙酰-亚氨基二苄基盐酸盐(Bonnecor,AWD 19-166,GS 015)在猫体内的药代动力学和药效学
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Electrophysiological effects of a new antiarrhythmic substance Bonnecor (AWD 19-166, GS 015) on mammalian myocardium.新型抗心律失常药物Bonnecor(AWD 19 - 166,GS 015)对哺乳动物心肌的电生理效应
Pharmazie. 1985 Dec;40(12):847-51.