(局部麻醉剂。VXII。2-和3-烷氧基取代苯氨基甲酸二碱式烷基酯的制备及其有效性。

Ceskoslovenska farmacie Pub Date : 1993-06-01
J Csöllei, L Búciová, J Cizmárik, L Kopácová
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引用次数: 0

摘要

在一系列24种2-和3-烷氧基取代苯氨基甲酸的二碱式烷基酯化合物中,使用了1-二丙基氨基-3-吡咯里迪诺(胡椒或过氢氮化氨基)-2-丙醇酯化醇。从药理学评价的结果可以看出,与可卡因和普鲁卡因的标准相比,这些化合物在表面和浸润麻醉方面具有很高的有效性指数。3-丁氧基苯基氨基甲酸的[1-二丙基氨基甲基]- 2-(胡椒碱)乙基]-酯在表面麻醉中显示出最大的效果,其活性比可卡因高180倍。[1-二丙基氨基甲基)-2-(吡咯烷酮)乙酯]戊氧基苯基氨基甲酸酯在浸润麻醉中的效果最好,其活性比标准普鲁卡因高250倍。所制备的化合物在浸润情况下比在表面麻醉情况下更有效。
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[Local anesthetics. VXII. Preparation and effectiveness of dibasic alkylesters of 2-, and 3-alkoxy-substituted phenylcarbamic acids].

In a series of 24 compounds of the type of dibasic alkylesters of 2-, and 3-alkoxy substituted phenylcarbamic acids, esterified alcohols 1-dipropylamino-3-pyrrolidino (piperidino or perhydroazepino)-2-propanol were used. It follows from the results of pharmacological evaluation that these compounds possess a high index of effectiveness in surface and infiltration anaesthesia compared to the standards of cocaine and procaine. Maximum effectiveness in surface anaesthesia was shown by [1-dipropylaminomethyl)-2- (piperidino)ethyl]-ester of 3-butoxyphenylcarbamic acids whose activity is as much as 180 times higher than that of cocaine. Maximum effectiveness in infiltration anaesthesia was shown by [1-dipropylaminomethyl)-2-(pyrrolidino)ethyl] ester of pentyloxyphenylcarbamic acid achieving an activity 250 times higher than that of standard procaine. The prepared compounds are more effective in the case of infiltration than in the case of surface anaesthesia.

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