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[多种ω-氨基酰基-3-甲酰氧基氨基二苯并氮杂䓬的化学结构与抗心律失常作用之间的关系]

[The relationship between the chemical structure and anti-arrhythmia action of a number of omega-aminoacyl-3-carbalcoxyaminodibenzazepines].

作者信息

Gritsenko A N, Lyskovtsev V V, Senova Z P, Skoldinov A P, Stark A, Wunderlich G, Poppe H, Barch R

出版信息

Farmakol Toksikol. 1990 May-Jun;53(3):30-2.

PMID:2387375
Abstract

The antiarrhythmic activity of 20 derivatives of dibenzazepine (the effects on the maximal effective rabbit heart auricle contraction rate, aconitine-induced arrhythmia in rats under or without anesthesia) was studied. It was shown that the most active compounds are those with carbethoxyamine group in position 3 in combination with dimethylamino- or diethylamino-acetyl groups in position 5 of dibenzazepine ring. 5-dimethyl-aminoacetyl-10,11-dihydro-5H-dibenz b, f azepine (GS-015, bonnecor) was selected for the further detailed investigation.

摘要

研究了二苯并氮杂䓬的20种衍生物的抗心律失常活性(对家兔离体心脏最大有效收缩速率的影响,对麻醉或未麻醉大鼠乌头碱诱发心律失常的影响)。结果表明,活性最强的化合物是那些在二苯并氮杂䓬环的3位带有乙氧羰基胺基团并在5位与二甲氨基或二乙氨基乙酰基结合的化合物。选择5-二甲氨基乙酰基-10,11-二氢-5H-二苯并[b,f]氮杂䓬(GS-015,邦尼可)进行进一步详细研究。

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