OBJECTIVE: To determine the subset of alpha 1-adrenoceptors mediating the functional abstraction of the prostate to noradrenaline. MATERIALS AND METHODS: Radioligand experiments were performed with membranes prepared from rat 1 fibroblasts transfected with rat alpha 1a, hamster alpha 1b or bovine alpha 1c adrenoceptor cDNA. Human prostatic tissue obtained from transurethral resection of the prostate with full informed consent was submitted to functional in vitro muscle strip experiments. RESULTS: The binding experiments defined the potential subtype selectivity of various antagonists. Using this information, it was possible to define the functionally important alpha 1-adrenoceptor subtype in the human prostate. CONCLUSION: This work reports the results of the first functional characterization of the alpha 1c-adrenoceptor subtype. The most functionally important alpha 1-adrenoceptor type in the human prostate appears to be the alpha 1c subtype. This finding may aid the development of prostate-selective adrenoceptor pharmacotherapy.
OBJECTIVE: To determine the subset of alpha 1-adrenoceptors mediating the functional abstraction of the prostate to noradrenaline. MATERIALS AND METHODS: Radioligand experiments were performed with membranes prepared from rat 1 fibroblasts transfected with rat alpha 1a, hamster alpha 1b or bovine alpha 1c adrenoceptor cDNA. Human prostatic tissue obtained from transurethral resection of the prostate with full informed consent was submitted to functional in vitro muscle strip experiments. RESULTS: The binding experiments defined the potential subtype selectivity of various antagonists. Using this information, it was possible to define the functionally important alpha 1-adrenoceptor subtype in the human prostate. CONCLUSION: This work reports the results of the first functional characterization of the alpha 1c-adrenoceptor subtype. The most functionally important alpha 1-adrenoceptor type in the human prostate appears to be the alpha 1c subtype. This finding may aid the development of prostate-selective adrenoceptor pharmacotherapy.