Studies on the Mechanism of Action of the Gastric H^+,K^+-ATPase Inhibitor SPI-447
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概要
- 論文の詳細を見る
3−Amino−5−methyl−2(2−methyl−3−thienyl)−imidazo[1, 2−a]thieno[3, 2−c]pyridine, SPI−447, is a potent gastric H+, K+−ATPase inhibitor, but a detailed mechanism of the inhibition is unknown.This study was designed to investigate the mechanism by which SPI−447 inhibits gastric H+, K+−ATPase.For this purpose, the inhibitory action of SPI−447 on gastric H+, K+−ATPase from porcine gastric mucosa was compared with that of omeprazole(an irreversible inhibitor)and SCH28080(a reversible inhibitor).All compounds produced dose−dependent inhibition of gastric H+, K+−ATPase, and the inhibitory intensities were increased under acidic conditions.The anti−H+, K+−ATPase actions of SPI−447 and SCH28080 were attenuated by dilution, but not influenced by glutathione pretreatment.In contrast, that of omeprazole was not influenced by dilution, but was suppressed by glutathione pretreatment.KCl addition reversed the inhibition of H+, K+−ATPase−mediated H+−transport by SPI−447 and SCH28080, but had no effect on that by omeprazole.The anti−gastric H+, K+−ATPase action of SPI−447 was additive with that of SCH28080.SPI−447 and SCH28080 had no effect on Na+, K+−ATPase activity.These findings indicated that the inhibitory mechanism of SPI−447 on gastric H+, K+−ATPase was similar to that of SCH28080, but different from that of omeprazole;i.e., 1)reversible, 2)SH−group independent, 3)K+−competitive, and 4)highly specific against gastric H+, K+−ATPase.
- 社団法人 日本薬理学会の論文
- 2000-01-01
著者
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ICHIHARA Toshio
Department of Experimental Pathology and Tumor Biology, Nagoya City University Graduate School of Me
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TANAKA Hironori
Department of Laboratory Medicine, Nagasaki University School of Medicine
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NARITA Mitsuhiro
Department of Urology, Shiga University of Medical Science
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YAMAZAKI Takashi
Department of Astrophysics, School of Science, Nagoya University
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Ichihara Toshio
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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TSUKIMI Yasuhiro
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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USHIRO Toshihisa
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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ISHIKAWA Harumi
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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HIRASE Jyoji
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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NISHIGAITO Toshiki
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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BANNO Kimiko
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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Narita Mitsuhiro
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Narita Mitsuhiro
Department Of Applied Pharmacology Kyoto Pharmaceutical University
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Banno Kimiko
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Ishikawa Harumi
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Hirase Jyoji
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Tanaka H
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Nishigaito Toshiki
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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TSUKIMI Yasuhiro
TRA Urology, Laboratory-4, Research Center Kyoto, Bayer Yakuhin Ltd.
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Tanaka Hironori
Department Of Applied Molecular Biosciences Graduate School Of Bioagricultural Sciences Nagoya Unive
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Yamazaki Takashi
Department Of Applied Chemistry Graduate School Of Engineering Tokyo University Of Agriculture And T
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Tsukimi Y
Tra Urology Laboratory-4 Research Center Kyoto Bayer Yakuhin Ltd.
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Tsukimi Yasuhiro
Department Of Applied Pharmacology Kyoto Pharmaceutical University
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Ushiro Toshihisa
Department Of New Drug Research Laboratories Technical Headquarters Shinnippon Pharmaceutical Inc
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Tsukimi Yasuhiro
Inflammation Drug Discovery Unit Pharmaceutical Research Division Takeda Pharmaceutical Company Limi
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ICHIHARA Toshio
Department of Earth and Space Science, Faculty of Science, Osaka University
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Yamazaki Takashi
Department of New Drug Research Laboratories, Technical Headquarters, Shinnippon Pharmaceutical, Inc
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