Tamsulosin: α_1 : Adrenoceptor Subtype : Selectivity and Comparison With Terazosin

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Author(s)

Abstract

Selectivity of tamsulosin and terazosin to functional α<SUB>1</SUB>-adrenoceptors was examined. Both drugs competitively inhibited the contractile responses to noradrenaline in different tissues where the responses were mediated through the α<SUB>1D</SUB>-, α<SUB>1B</SUB>- or α<SUB>1L</SUB>-subtype. Together with the affinities obtained in the binding study with cloned (α<SUB>1a</SUB>, α<SUB>1b</SUB>, α<SUB>1d</SUB>) and native (α<SUB>1A</SUB> and α<SUB>1B</SUB>) subtypes, the selectivity of tamsulosin was α<SUB>1A</SUB>>α<SUB>1L</SUB>, α<SUB>1D</SUB>>α<SUB>1B</SUB>. Terazosin had lower affinity at various subtypes than tamsulosin, but showed relatively high selectivity to the α<SUB>1D</SUB>-subtype. In the human prostate, tamsulosin was more than 30-fold higher in affinity than terazosin in functional and binding studies.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 78(3), 331-335, 1998-11-01

    The Japanese Pharmacological Society

References:  26

Codes

  • NII Article ID (NAID)
    10008681276
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    ART
  • ISSN
    00215198
  • NDL Article ID
    4610822
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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