Antioxidative Action of the β-Adrenoceptor Antagonist Bopindolol and Its Metabolite 18-502
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概要
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The antioxidative effects of β-adrenoceptor antagonists and related compounds were investigated. Among the β-adrenoceptor antagonists, the agents with a potent membrane-stabilizing activity such as bopindolol and propranolol strongly inhibited the hydrogen peroxide (H<SUB>2</SUB>O<SUB>2</SUB>)-induced lipid peroxidation of liver microsomes. Fifty percent inhibition concentration values for the lipid peroxidation of bopindolol, 18-502 (metabolite of bopindolol) and propranolol were calculated to be 1.8 μM, 10 μM and 2.3 μM, respectively. The same potency order of the agents for the inhibition of lipid peroxidation was observed in rat heart homogenates. Furthermore, cytochrome P-450-catalyzing lipid peroxidation in microsomes and H<SUB>2</SUB>O<SUB>2</SUB>-induced lipid peroxidation in coronary arteries or cardiac muscles of pigs were also inhibited by bopindolol, whereas propranolol was less effective. Bopindolol and 18-502, but not propranolol, scavenged a stable free radical 1, 1-diphenyl-2-picrylhydrazyl. Thus it was concluded that bopindolol that has membrane-stabilizing and radical scavenging activities is a more potent antioxidant than propranolol and may produce a beneficial effect for the treatment of ischemic cardiac diseases.
- 社団法人 日本薬理学会の論文
- 1995-07-01
著者
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Aniya Yoko
Laboratory of Molecular Genetics and Pharmacology, School of Health Sciences, Faculty of Medicine, U
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Naito Akira
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
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Aniya Y
Univ. Ryukyus Okinawa Jpn
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Aniya Yoko
Laboratory Of Functional And Molecular Pharmacology Graduate School Of Medicine University Of The Ry
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SAKANASHI Mayuko
Department of Pharmacology, School of Medicine, Faculty of Medicine, University of the Ryukyus
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Sakai M
Hokkaido Univ. Sapporo Jpn
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Sakai M
Olympus Optical Co. Ltd. Tokyo
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Sakai M
Univ. Tokyo Tokyo Jpn
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Sakai Masayuki
Department Of Hospital Pharmacy Faculty Of Medicine University Of The Ryukyus
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Sakanashi M
Department Of Pharmacology School Of Medicine Faculty Of Medicine University Of The Ryukyus
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Sakanashi Matao
Department Of Pharmacology:2nd Department Of Internal Medicine:school Of Medicine Faculty Of Medicin
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Aniya Yoko
琉球大学 保健
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FONG Kun
Laboratory of Physiolgy and Pharmacology, School of Health Sciences, University og the Ryukyus
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NAITO Akira
Laboratory of Physiolgy and Pharmacology, School of Health Sciences, University og the Ryukyus
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SAKANASHI Matao
Resoarch Center of Comprehensive Medicine, University of the Ryukyus
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Naito Akira
Department Of Anatomy Shinshu University School Of Medicine
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Fong Kun
Laboratory Of Physiolgy And Pharmacology School Of Health Sciences University Og The Ryukyus
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