Gritsenko A N, Lyskovtsev V V, Senova Z P, Skoldinov A P, Stark A, Wunderlich G, Poppe H, Barch R
Farmakol Toksikol. 1990 May-Jun;53(3):30-2.
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.
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。