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Abstract
1. The present study was designed to assess the displacement potencies of tamsulosin to 3H-prazosin bindings in two α 1-adrenoceptor (AR) subtypes (α 1H and α 1L) in bovine prostate, rat heart and brain compared with those of amosulalol, labetalol, ketanserin, clonidine and propranolol. 2. The p K i values of tamsulosin to α 1H and α 1L subtypes in bovine prostate were 9.13 and 8.99 and these values were almost the same as those of prazosin. On the other hand, low p K i binding values of amosulalol, labetalol, ketanserin, clonidine and propranolol to these subtypes were observed. 3. Low p K i values of tamsulosin to α 2- and β-ARs and muscarinic and 5HT 2 receptors in the rat brain were observed. 4. These results suggest that tamsulosin has high affinities to α 1L-AR subtypes in bovine prostate and rat hearts as well as α 1H-AR subtypes, implying an inhibitory effect of this drug on the contraction of the prostate.
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