The increase in .BETA.-adrenergic receptors in lymphocytes following treatment with xamoterol.

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概要

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• Xamoterol (100mg b.d.), a β<SUB>1</SUB>-adrenergic partial agonist, was given orally for 7 days to 8 healthy volunteers and to 8 patients with heart failure.β-adrenoceptors in lymphocytes were determined by radioligand-binding assay using <SUP>125</SUP>I-iodocyanopindolol before and after the administration of xamoterol.<BR>The values of density (B<SUB>max</SUB>) and affinity (K<SUB>d</SUB>) of the β-adrenoceptors were lower in the patients with heart failure than in the healthy volunteers (B<SUB>max</SUB>=931±214 vs 1466± 373 sites/cell, and K<SUB>d</SUB>=0.60±0.11 vs 1.07±0.14 nM).During treatment with xamoterol, the values of B<SUB>max</SUB> (7, 169±3, 768 and 7, 749±3, 807 sites/cell) and K<SUB>d</SUB> (6.01±3.84 and 9.06±4.66 nM) increased strikingly (P<0.01) in both groups.Following withdrawal of the treatment, the values of B<SUB>max</SUB> and K<SUB>d</SUB> decreased in both groups, but B<SUB>max</SUB> of the patients with heart failure remained higher (1, 385±457 sites/cell, P<0.05) than the pre-treatment level.Blood pressure rose slightly in the patients with heart failure during treatment with xamoterol, but heart rate and fractional shortening on echocardiography were unaffected.<BR>In conclusion, β-adrenoceptors in lymphocytes were up-regulated during treatment with xamoterol without deterioration of cardiac function in the patients with heart failure because of the β-agonist and β-antagonist activities of the drug.

• 一般社団法人 日本臨床薬理学会の論文

著者

• Shibata Akira

  First Department Of Internal Medicine Niigata University Niigata Case Western Reserve University

• Nagatomo Takafumi

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Hirokawa Yoichi

  First Department Of Medicine Niigata University School Of Medicine

• Tsuchihashi Hiroshi

  Department Of Pharmacology Niigata College Of Pharmacy

• Suzuki Kaoru

  First Department Of Internal Medicine Niigata University School Of Medicine

• WATANABE Ken-ichi

  Division of Cardiology, Tsubame Rosai Hospital

• SUZUKI Kaoru

  First Department of Internal Medicine, Niigata University School of Medicine

• HIROKAWA Yoichi

  First Department of Internal Medicine, Niigata University School of Medicine

• WATANABE Ken-ichi

  Division of Cardiology, Kuwana Hospital

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