Selectivity of bunitrolol for .BETA.1- and .BETA.2-adrenergic receptors and 5HT1B-receptors: Assessment by biphasic scatchard plots and biphasic displacement curve analysis with 125I-iodocyanopindolol and 3H-CGP12177.
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概要
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The preference by bunitrolol for β<SUB>1</SUB> and β<SUB>2</SUB>-adrenoceptors of the rat brain, heart and/or lung was assessed by the radioligand binding assay method with <SUP>125</SUP>I-iodocyanopindolol (<SUP>125</SUP>I-ICYP) or <SUP>3</SUP>H-CGP12177. Scatchard plots of <SUP>125</SUP>I-ICYP binding in the presence of bunitrolol were found to be non-linear. The inhibition constants (K<SUB>j</SUB>) of bunitrolol for high (β<SUB>2</SUB>-) and low affinity sites (β<SUB>1</SUB>-) were: 0.42±0.16 nM for β<SUB>1</SUB> and 3.55±1.61 nM for β<SUB>2</SUB> (β<SUB>1</SUB> > β<SUB>2</SUB>), respectively. Displacement experiments conducted with the preparations of the rat brain using <SUP>125</SUP>I-ICYP or with the preparations of the rat heart using <SUP>3</SUP>H-CGP12177 yielded K<SUB>j</SUB> values for bunitrolol of 0.53±0.20 (β<SUB>1</SUB>) and 2.37±0.78 (β<SUB>2</SUB>) nM for <SUP>125</SUP>I-ICYP binding and 2.01±0.38 (β<SUB>1</SUB>) and 12.67±6.54 (β<SUB>2</SUB>) nM for <SUP>3</SUP>H-CGP12177 binding. In addition, the K<SUB>j</SUB> value for 5HT<SUB>1B</SUB>-receptors assessed in displacement experiments conducted with <SUP>125</SUP>I-ICYP in the presence of 30 μMI-metoprolol in the rat brain was 10.54±5.92 nM. Thus, bunitrolol is a β<SUB>1</SUB>-selective antagonist.
- 公益社団法人 日本薬理学会の論文
著者
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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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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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