[Preparation and pharmacologic profile of derivatives of alkoxyphenylcarbamic acid with potential effects on the cardiovascular system].

Ceskoslovenska farmacie Pub Date : 1993-12-01
E Racanská, A Kulcsár, I Tumová, J Csöllei, L Búciová
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Abstract

In a systematic study of the relationship between the chemical structure and beta-adrenolytic activity, eleven derivatives of the 4-alkoxysubstituted phenylcarbamic acids were prepared. The beta-adrenolytic efficiency of the compounds was studied in the isolated spontaneously beating guinea-pig atria and expressed as pA2 values against isoprenaline tachycardia. Negative chronotropic and antidysrhythmic activity were also evaluated. All of the compounds studied were local anesthetically active and their indexes of efficiency were 3-50 fold higher in comparison with standards cocaine and procaine. The acute toxicity of the compounds was within the acceptable limits.

[对心血管系统有潜在影响的烷氧苯氨基甲酸衍生物的制备和药理学研究]。
为了系统地研究4-烷氧基取代苯氨基甲酸的化学结构与β -肾上腺素活性之间的关系,制备了11种4-烷氧基取代苯氨基甲酸衍生物。在离体自然跳动豚鼠心房中研究了化合物的β -肾上腺素溶解效率,并以pA2值对异丙肾上腺素心动过速表示。负变时性和抗节律障碍活性也进行了评估。所研究的化合物均具有局部麻醉活性,其效率指数比标准可卡因和普鲁卡因高3-50倍。化合物的急性毒性在可接受范围内。
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