Binding characteristics of 3H-CGP12177 to .BETA.-adrenoceptors in rat myocardial membranes.
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概要
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The present study was designed to examine the selectivity of <SUP>3</SUP>H-CGP-12177 (4-(3-t-butylamino-2-hydroxypropoxy)-[5, 7-<SUP>3</SUP>H]benzimidazole-2-one hydrochloride) for β<SUB>1</SUB>- and β<SUB>2</SUB>-adrenergic receptors by the Scatchard and the displacement analysis. The plots of specific binding obtained from the Scatchard analysis using <SUP>3</SUP>H-CGP12177 for the rat myocardium membrane were uniphasic when the non-specific binding was detemined by the use of 10 μM I-propranolol, and the K<SUB>d</SUB> and B<SUB>max</SUB> values were 408.53±67.20 pM and 12.27±0.83 fmoles/mg protein, respectively. On the other hand, two binding sites were observed in the displacement curve when I-metoprolol was used as a competitor. The existence of these two binding sites implied the selectivity of <SUP>3</SUP>H-CGP12177 to β-adrenoceptors because <SUP>3</SUP>H-CGP12177 was 1.8-fold more selective towards β<SUB>1</SUB>-adrenoceptors than β<SUB>2</SUB>-adrenoceptors. In addition, these two binding sites could be regarded as β<SUB>1</SUB>-and β<SUB>2</SUB>-adrenergic receptors from the evaluation of the binding characteristics of β-adrenoceptors by the displacement analysis using β-selective antagonists. Thus, <SUP>3</SUP>H-CGP12177, a hydrophilic radioligand, was useful for the binding assay of β-adrenoceptors in rat myocardial membranes.
- 公益社団法人 日本薬理学会の論文
著者
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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YOKOYAMA Harunobu
Department of Pharmacology, Niigata College of Pharmacy
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