Simultaneous Differentiation of Three Opiate Receptor Subpopulations by Computer Modelling

Abstract

[³H]-(−)-bremazocine was displaced from guinea-pig brain membrane homogenates by three compounds having different specificity to opiate receptor subpopulations. A three site receptor model showed the best fit of the calculated to the measured value for the opiate mu (DAla², MePhe⁴, Gly(ol)⁵-enkephalin) and the delta specific compound (DAla², DLeu⁵-enkephalin). Computer modelling of data from displacement curves with the opiate kappa specific compound U-50.488H favored a two site receptor model.