Tamsulosin: .ALPHA.1-Adrenoceptor Subtype-Selectivity and Comparison With Terazosin.

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  • Tamsulosin:α1-Adrenoceptor Subtype-Selectivity and Comparison With Terazosin
  • Tamsulosin アルファ1-Adrenoceptor Subtype-S
  • Tamsulosin: ai-adrenoceptor subtype-selectivity and comparison with terazosin

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Abstract

Selectivity of tamsulosin and terazosin to functional α1-adrenoceptors was examined. Both drugs competitively inhibited the contractile responses to noradrenaline in different tissues where the responses were mediated through the α1D-, α1B- or α1L-subtype. Together with the affinities obtained in the binding study with cloned (α1a, α1b, α1d) and native (α1A and α1B) subtypes, the selectivity of tamsulosin was α1A>α1L, α1D>α1B. Terazosin had lower affinity at various subtypes than tamsulosin, but showed relatively high selectivity to the α1D-subtype. In the human prostate, tamsulosin was more than 30-fold higher in affinity than terazosin in functional and binding studies.

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