Inhibitory Effects of Bifemelane on Brain Ca^<2+> Channel Subtypes Expressed in Xenopus Oocytes
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概要
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Effects of the cerebroprotective agent bifemelane on voltage-dependent Ca2+ channel currents were evaluated in Xenopus oocytes expressing specific Ca2+-channel subtypes. Extracellular perfusion of bifemelane showed a dose-dependent blocking action on both N-type and Q-type Ca2+ channels, but not on cardiac L-type Ca2+ channels expressed in the oocytes, and the inhibitory action on Q-type current was stronger than that on N-type current. The time course of inhibition by bifemelane was comparatively slow; a 20-min perfusion with 1 μM bifemelane was required to reduce the amplitude of the Q-type current to 80% of the control level. When bifemelane was applied intracellularly, the potency and time-course of inhibition was equivalent to that caused by the perfusion of bifemelane. The bifemelane-induced inhibition was voltage-dependent but not use-dependent in Q-type channels since it was apparent at more depolarized potentials but not influenced by the interval of depolarization. These results suggest that bifemelane inhibits the opening of the specific Ca2+ channels located at nerve terminals to suppress excessive neurotransmitter release from neurons in some pathophysiological conditions such as ischemia.
- 社団法人 日本薬理学会の論文
著者
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Akaike A
Department Of Pharmacology Graduate School Of Pharmaceutical Sciences Kyoto University
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Akaike Akinori
京都大学 薬学研究科生体機能解析学
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Akaike A
Dep. Of Pharmacology Graduate School Of Pharmaceutical Sciences Kyoto Univ. Jpn
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Akaike Akinori
京都薬科大学 病態生理
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Akaike Akinori
Department Of Pharmacology Graduate School Of Pharmaceutical Sciences Kyoto University
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KANEKO Shuji
Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University
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Akaike Akinori
Department Of Pharmaceutical Science Kyoto University Graduate School Of Pharmacology
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SATOH Masamichi
Department of molecular Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto university
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Kaneko Shuji
Department Of Neuropharmacology Graduate School Of Pharmaceutical Sciences Kyoto University
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Kaneko Shuji
Department Of Applied Biological Chemistry Graduate School Of Agricultural Science Kobe University
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Satoh Masamichi
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Science Kyoto University
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KINOSHITA Mariko
Departments of Pharmacotogy, Graduate School of Pharmaceutical Sciences, Kyoto University
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YASUNO Tohru
Departments of Pharmacotogy, Graduate School of Pharmaceutical Sciences, Kyoto University
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YADA Nobumichi
Departments of Pharmacotogy, Graduate School of Pharmaceutical Sciences, Kyoto University
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Yasuno Tohru
Departments Of Pharmacotogy Graduate School Of Pharmaceutical Sciences Kyoto University
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Yada Nobumichi
Departments Of Pharmacotogy Graduate School Of Pharmaceutical Sciences Kyoto University
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Kinoshita Mariko
Departments Of Pharmacotogy Graduate School Of Pharmaceutical Sciences Kyoto University
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Satoh Masamichi
Department Of Hygiene And Preventive Medicine Faculty Of Medicine Saitama Medical School
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Akaike Akinori
Department of Neuropharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University
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Yasuno Tohru
Department of Biopharmaceutics, Kyoto Pharmaceutical University
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