Studies of Local AnaestheticsCL. Models of Dependence of Local Anaesthetic Effectiveness of Basic Esters of Alkoxy-substituted Phenylcarbamic Acids on the Capacity Factor k’

Overview

On the basis of proposed six models of the dependence of local anaesthetic effectiveness of series ofalkoxysubstituted derivatives of phenylcarbamic acid, this activity was studies in dependence onthe 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 thevalue of the decadic logarithm of surface or infiltration local anaesthetic activity, Cx the coefficientcharacterizing the nitrogenous base, Ci the coefficient characterizing the individual alkoxygroups,and k’ the capacity factor from HPLC.

Key words:
local anaesthetic activity – derivatives of alkoxyphenylcarbamic acid – capacityfactor k’ – dependence