Effects of bunitrolol on adrenergic and serotonergic receptors.
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概要
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To assess the importance of anti-adrenergic and anti-serotonergic activities of bunitrolol for its efficacy as an antihypertensive and antianginal agent, effects of this substance on the binding of adrenergic and serotonergic agents to the respective receptors of the rat brain, rat heart, dog brain, and/or dog aorta were examined using the radioligand binding assay methods. In addition, the pA<SUB>2</SUB> values of bunitrolol as an antagonist against the positive chronotropic and inotropic actions (β<SUB>1</SUB>-adrenoceptor) of isoproterenol were also determined by pharmacological methods using the isolated guinea pig atria. To assess the specificity, pA<SUB>2</SUB> values were also obtained in the isolated trachea (β<SUB>2</SUB>-adrenoceptor) using isoproterenol as an agonist and in the isolated aorta from the guinea pig and the rat using phenylephrine as an agonist (α<SUB>1</SUB>-adrenoceptor). A strong inhibition by bunitrolol of <SUP>3</SUP>H-dihydroalprenolol (<SUP>3</SUP>H-DHA) binding to β-adrenoceptors was observed, while the inhibition of <SUP>3</SUP>H-prazosin binding to α<SUB>1</SUB>-adrenoceptors, <SUP>3</SUP>H-serotonin binding to 5HT<SUB>1</SUB>-receptors. <SUP>3</SUP>H-p-aminoclonidine binding to α<SUB>2</SUB>-adrenoceptors, and <SUP>3</SUP>H-ketanserin binding to 5HT<SUB>2</SUB>-receptors were found to be very weak. The rank order of antagonistic potencies of bunitrolol against the adrenergic receptors as asessed with pA<SUB>2</SUB> values were β<SUB>1</SUB>>β<SUB>2</SUB>>>α<SUB>1</SUB>. From these two different types of experiments, it is clear that the antihypertensive and antianginal effects of bunitrolol are mainly due to its β-blocking actions, with the α<SUB>1</SUB>-blocking action of this drug playing a minor role.
- 公益社団法人 日本薬理学会の論文
著者
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Ohta Hideo
Department Of Surgery Sakai Municipal Hospital
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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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KAWADA Tomie
Department of Clinical Pharmacology, Faculty of Pharmacy, Musashino University
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AONO Junichiro
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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KAWADA Tomie
Department of Pharmacology, Niigata University School of Medicine
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OHTA Hideo
Department of Pharmacology, Niigata University School of Medicine
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