Pharmacological Characteristics of Inhibitory Action of the Selective α_1-Antagonist JTH-601 on the Positive Inotropic Effect Mediated by α_1-Adrenoceptors in Isolated Rabbit Papillary Muscle

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Influence of JTH-601 [N-(3-hydroxy-6-methoxy-2, 4, 5-trimethylbenzyl)-N-methyl-2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethylamine hemifumarate], a selective α<SUB>1</SUB>-adrenoceptor antagonist, on α<SUB>1</SUB>-mediated positive inotropic effect (PIE) was studied in isolated rabbit papillary muscle (1 Hz at 37°C). JTH-601 (0.1-10 μM) shifted the concentration-response curve (CRC) for PIE of phenylephrine mediated by α<SUB>1</SUB>-adrenoceptor (with timolol at 1 μM) to the right and downward. In the presence of 100 nM WB 4101, an α<SUB>1A</SUB> antagonist, the shift to the right disappeared and JTH-601 (1-3 μM) shifted CRC for phenylephrine downward. The antagonistic action of JTH-601 was unchanged by 100 nM (+)-niguldipine, another α<SUB>1A</SUB> antagonist. Following pretreatment with 10 μM chloroethylclonidine, an α<SUB>1B</SUB> antagonist, the shift of CRC for phenylephrine to the right disappeared and JTH-601 (3-10 μM) shifted CRC downward. Antagonistic action of JTH-601 (3 μM) was unaltered by 100 nM BMY 7378, an α<SUB>1D</SUB> antagonist. JTH-601 (10 μM) had no effect on β-mediated PIE of isoproterenol. These results indicate that JTH-601 exerts an inhibitory action on α<SUB>1</SUB>-mediated PIE through antagonism of α<SUB>1A</SUB>- and/or α<SUB>1B</SUB>-adrenoceptors in rabbit ventricular myocardium. As an α<SUB>1</SUB> antagonist, JTH-601 is much less potent in rabbit ventricular muscle than in smooth muscle.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 84(3), 301-309, 2000-11-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008186202
  • 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
    5586895
  • 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  CJP引用  NDL  J-STAGE 
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