BINDING CHARACTERISTICS OF <SUP>3</SUP>H-DIHYDROALPRENOLOL TO β-ADRENOCEPTORS OF RAT HEART TREATED WITH NEURAMINIDASE
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概要
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Binding characteristics of the β-blockers and β-agonists with the β-adrenoceptors were investigated in <SUP>3</SUP>H-dihydroalprenolol (<SUP>3</SUP>H-DHA) binding to rat heart membranes treated with neuraminidase. When 60% of the total sialic acid content in the membranes was removed, reproducibility of the binding assay became much better than was attainable without neuraminidase treatment, and the maximum density of β-adrenoceptors was increased. These data suggest that the binding of the test compounds with the β-adrenergic receptors in cardiac muscle was under the influence of the sialic acid of the glycocalyx of the membrane. The <SUP>3</SUP>H-DHA binding sites in membranes treated with neuraminidase showed a strict stereo-specificity when tested with propranolol. The ranking order of inhibition of β-antagonists or agonists is: dl-propranolol > oxprenolol > alprenolol > pindolol > YM-09538 > labetalol > acebutolol > atenolol > metoprolol > sotalol > butoxamine > practolol as antagonists or l-isoproterenol > I-epinephrine > I-norepinephrine as agonists. A good correlation (r=0.91, P < 0.001) was observed between the K; values observed by the present binding assay and the pA<SUB>2</SUB> observed in the guinea-pig atria relative to the positive inotropic effect by Bieth et al. (Br. J. Pharmacol. 68, 563-569, 1980), indicating that the present method will be useful for screening new β-adrenergic receptor antagonists or agonists.
- 社団法人 日本薬理学会の論文
著者
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NAGATOMO Takafumi
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
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IMAI Shoichi
Department of Pharmacology, Niigata University School of Medicine
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Nagatomo T
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie
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TSUCHIHASHI HIROSHI
Department of Surgery, Department of Medicine, Shiga University of Medical Science
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Imai Shoichi
Department Of Phamacology Niigata University School Of Medicine
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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SASAKI Miyuki
Department of Pharmacology, Niigata College of Pharmacy
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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Namikawa Tomoko
Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.
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