Artem'eva O V, Napalkova S M, Kostin Ia V, Skachilova S Ia
Department of Pharmacology, Mordovian State University, Saransk, Russia.
Eksp Klin Farmakol. 1999 Mar-Apr;62(2):22-4.
Experiments were conducted on models of early occlusion and reperfusion arrhythmias in cats to study the antiarrhythmic activity of trimecain, its morpholine analogue (MPT), and MPT derivatives containing glycine, magnesium salt of aspartic acid, and N-acetylglutaminic acid. All the compounds were injected in doses of 5% of LD50. A 22.5 mg/kg dose of trimecain prevented cardiac rhythm disorders after occlusion of the coronary arteries as well as after restoration of the coronary blood flow. Replacement of the diethyl group in the structure of trimecain by the morpholine ring led to diminution of antiarrhythmic activity, and MPT in a dose of 28.0 mg/kg, in distinction from the former, had no effect on the frequency of the occurrence of early occlusion arrhythmias and the duration of reperfusion arrhythmias. Introduction of amino acids as an anion into the MPT structure raised the antiarrhythmic activity of the last named.
在猫的早期闭塞和再灌注心律失常模型上进行了实验,以研究曲美卡因、其吗啉类似物(MPT)以及含有甘氨酸、天冬氨酸镁盐和N - 乙酰谷氨酰胺酸的MPT衍生物的抗心律失常活性。所有化合物均以半数致死量(LD50)的5%剂量注射。22.5mg/kg剂量的曲美卡因可预防冠状动脉闭塞后以及冠状动脉血流恢复后的心律失常。曲美卡因结构中的二乙基团被吗啉环取代导致抗心律失常活性降低,与前者不同,28.0mg/kg剂量的MPT对早期闭塞性心律失常的发生频率和再灌注性心律失常的持续时间没有影响。将氨基酸作为阴离子引入MPT结构可提高其抗心律失常活性。