Receptor Subtypes Involved in the α_1-Adrenoceptor Mediated Increase in ^<86>Rb^+ Efflux from the Rat Heart

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The aim of this study was to determine the involvement of the different α<SUB>1</SUB>-adrenoceptor subtypes in the α<SUB>1</SUB>-adrenoceptor mediated increase in <SUP>86</SUP>Rb<SUP>+</SUP> efflux from rat hearts. Isolated hearts were perfused in the presence of a, β-adrenoceptor antagonist (1 μM timolol). After loading with <SUP>86</SUP>Rb<SUP>+</SUP>, the efflux was measured during α1-adrenoceptor stimulation by phenylephrine (30μM). Phenylephrine increased the <SUP>86</SUP>Rb<SUP>+</SUP> efflux by about 30%. Pretreatment with the preferentially α<SUB>1B</SUB>-adrenoceptor inhibitor chloroethylclonidine (CEC), reduced the response to phenylephrine by about 50%. The preferential α<SUB>1D</SUB>-adrenoceptor inhibitor BMY 7378 inhibited the response to phenylephrine by 35%, with a pK<SUB>I</SUB>=8.4 (95% C.I. 8.2-8.6). The response was sensitive to the preferential α<SUB>1A</SUB>-adrenoceptor inhibitors (+)niguldipine, 5-methylurapidil (5-MU) and WB-4101 at relatively high concentrations, and 5-MU inhibited the response with a pKI = 7.7 (95% C.I. 7.2-8.0) in CEC pretreated hearts. In conclusion, the phenylephrine stimulated increase in <SUP>86</SUP>Rb<SUP>+</SUP> efflux in the rat heart is not specifically linked to only one of the α<SUB>1</SUB>-adrenoceptor subtypes, but involves the α<SUB>1B</SUB> and the α<SUB>1D</SUB>-adrenoceptor subtypes, and probably the α<SUB>1A</SUB>-adrenoceptor subtype as well.

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  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 75(2), 171-178, 1997-10-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008189671
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    00215198
  • NDL 記事登録ID
    4326415
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  NDL  J-STAGE 
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