Reversed-Phase Chromatographic System as a Model for Characterizing the Offset Rate of Action of Azidomorphines in Guinea-Pig Ileum

Abstract

Abstract The relationship between the offset rate of action and physicochemical properties of asidomorphines was investigated. The offset rate of action of 12 compounds was measured in isolated preparations of guinea-pig ileumo. Physicochemical properties of asidomorphines were characterised by their hydrophobicity parameters, determined by reversed-phase high-performance liquid chromatography and by their activity in lowering surface tension. The offset rate of action of azidomorphine derivatives in guinea-pig ileum proved to be inversely related to their hydrophobicity, as shown by correlation analysis. A reversed-phase chromatographic system was developed which appears to be suitable for the estimation of the offset rate of action of azidomorphines.