Characteristics of <SUP>125</SUP>I-lodocyanopindolol Binding to β-Adrenergic and Serotonin-1B Receptors of Rat Brain: Selectivity of β-Adrenergic Agents
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概要
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The present study was designed to examine the specificity of β-adrenergic antagonists for β<SUB>1</SUB>, β<SUB>2</SUB>-adrenergic and 5HT<SUB>1B</SUB>-serotonergic receptors by the competitive interaction with <SUP>125</SUP>I-iodocyanopindolol (<SUP>125</SUP>I-ICYP) as a radioligand. The β<SUB>1</SUB>-adrenoceptors were preferred by acebutolol, atenolol, betaxolol, practolol, and I-, dl and d-metoprolol, while butoxamine and ICI-118, 551 preferred β<SUB>2</SUB>-adrenoceptors. The selectivities of these β<SUB>1</SUB> and β<SUB>2</SUB>-antagonists are well-known, but alprenolol which is known as a non-selective antagonist was 7.2-fold more selective for the β<SUB>2</SUB>-adrenoceptors in the present study. All β-antagonists used were more selective towards β-adrenoceptors as compared with 5HT<SUB>1B</SUB>-receptors. Good correlations were observed between the potencies of β-adrenoceptor antagonists for inhibition of <SUP>125</SUP>I-ICYP binding to β<SUB>1</SUB>- and β<SUB>2</SUB>-adrenoceptor sites and their potencies for inhibiting the binding of the same radioligand to 5HT<SUB>1B</SUB>-serotonergic receptor sites. These results suggest that β-adrenoceptor antagonists can bind to β-adrenoceptors and 5HT<SUB>1B</SUB>-receptors.
著者
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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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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NAKASHIMA Yasuo
Department of Pharmacology, Niigata College of Pharmacy
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