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[局部麻醉药的研究。CL。烷氧基取代苯基氨基甲酸酯类局部麻醉药效能对容量因子k'的依赖性模型]

[Studies of local anesthetics. CL. Models of the dependence of local anesthetic effectiveness of basic esters of alkoxy-substituted phenylcarbamic acids on capacity factor k'].

作者信息

Cizmárik J, Lehotay J, Bednáriková A, Hrobonová K

机构信息

Katedra farmaceutickej chémie, Farmaceutickej fakulty, Univerzity Komenského, Bratislava.

出版信息

Ceska Slov Farm. 1999 Nov;48(6):276-80.

PMID:10748746
Abstract

On the basis of proposed six models of the dependence of local anaesthetic effectiveness of series of alkoxysubstituted derivatives of phenylcarbamic acid, this activity was studies in dependence on the capacity factor k' as the parameter of lipophilicity. The most suitable models proved to be y = (Cx + Ci).k' for surface anaesthesia, and y = Cx + Ci log k' for infiltration anaesthesia, y being the value of the decadic logarithm of surface or infiltration local anaesthetic activity, Cx the coefficient characterizing the nitrogenous base, Ci the coefficient characterizing the individual alkoxygroups, and k' the capacity factor from HPLC.

摘要

基于所提出的苯氨基甲酸系列烷氧基取代衍生物局部麻醉效果依赖性的六种模型,研究了该活性与作为亲脂性参数的容量因子k'之间的关系。结果表明,对于表面麻醉,最合适的模型是y = (Cx + Ci).k';对于浸润麻醉,最合适的模型是y = Cx + Ci log k',其中y为表面或浸润局部麻醉活性的常用对数值,Cx为表征含氮碱的系数,Ci为表征各个烷氧基的系数,k'为高效液相色谱法中的容量因子。

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Ceska Slov Farm. 1999 Nov;48(6):276-80.
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