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Vol. 280, Issue 1, 1-5, 1997

Effects of Tamsulosin Metabolites at Alpha-1 Adrenoceptor Subtypes

Katsunari Taguchi, Minori Saitoh, Shuichi Sato, Masaharu Asano and Martin C. Michel

Department of Medicine (K.T., M.C.M.), University of Essen, 45122 Essen, Germany and Yamanouchi Pharmaceutical Co. (M.S., S.S., M.A.), Tokyo, Japan

We have investigated the affinity and selectivity of tamsulosin and its metabolites, M1, M2, M3, M4 and AM1, at the tissue and the cloned alpha-1 adrenoceptor subtypes in the radioligand binding and the functional studies. In the radioligand binding studies, the compounds competed for [3H]prazosin binding to the rat liver and kidney alpha-1 adrenoceptors, with the rank order of potency tamsulosin approx  M4 > M1 > M2 approx  M3 >> AM1 with the latter having a negligible affinity. All compounds differentiated cloned alpha-1 adrenoceptor subtypes with the rank order of potency of alpha-1A >=  alpha-1D > alpha-1B, except for M4 which had the highest affinity for the alpha-1D adrenoceptor. The compounds also concentration-dependently antagonized phenylephrine-induced contractions in the rabbit aorta and prostate. The resulting apparent pA2 values were very similar to those at the cloned rat alpha-1A adrenoceptor. We conclude that most tamsulosin metabolites are high potency antagonists at the alpha-1 adrenoceptors and retain the alpha-1A over the alpha-1B adrenoceptor selectivity of tamsulosin.

Copyright © by The American Society for Pharmacology and Experimental Therapeutics


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