Binding and functional properties of alpha1 adrenoceptors in different regions of the human prostate.

Abstract

The objective of the present study was to determine the density and functional properties of alpha 1 adrenoceptors in different regions of the human prostate. Binding and functional studies were performed on eight different topographical regions of the prostate. The contractile response (gm. force/mm.2 cross-sectional area [CSA]) was determined at varying concentrations of phenylephrine, and saturation experiments were performed at seven different concentrations of 125I-Heat. The maximal response to phenylephrine (Emax) ranged from 0.067 to 0.272 gm. force/mm.2 The CSA and the EC50 ranged from 25 to 41 microM. The differences between EC50 and Emax were not significantly different among the eight prostatic regions. A 1.8-fold difference between the Emax for peripheral and central regions of the prostate was statistically significant (p = 0.04). The equilibrium dissociation constant (Kd) of 125I-Heat and the receptor density Bmax were determined from the Scatchard plots. The mean Kd and Bmax ranged from 0.15 to 0.26 nM. and 0.30 to 0.72 fmol. per mg. wet weight, respectively. There were no statistically significant differences between mean Kd and mean Bmax for the eight prostatic regions. The 1.7-fold difference between central and peripheral mean Bmax was not statistically significant (p = 0.07). A direct relationship was not observed between phenylephrine mean Emax and mean Bmax. The present study demonstrates regional differences of the binding and functional properties of prostatic alpha 1 adrenoceptors in the human prostate. These regional differences must be taken into account when investigating the pharmacologic and physiologic properties of the prostate.