α1-Adrenoceptor Subtypes in Bovine Prostate

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Abstract
The object of this study was to examine the existence and characteristics of α1-adrenoceptor subtypes in the bovine prostate using the radioligand binding assay method. [3H]Prazosin was used as the radioligand and its binding sites in bovine prostate were classified into two subtypes. One subtype showed a high affinity (α1High, Kd: 101·1 Pm and Bmax: 11·8 fmol (mg protein)−1) and the other had a low affinity (α1Low, Kd: 3371·4 Pm and Bmax: 50·5 fmol (mg protein)−1). Although the same pKi values of clorethylclonidine, p-aminoclonidine, benoxathian and dibenamine to both α1High and α1 Low binding sites in bovine prostate tissue were observed, other α1 antagonists used in this study had different pKi values for the two α1-adrenoceptor subtypes. The existence and binding characteristics of α1-adrenoceptor subtypes in bovine prostate were clarified. It is possible that agents selective for one site may contribute to the development of better drugs for the treatment of bladder outlet obstructions of men with benign prostatic hyperplasia.

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