Stereoselectivity and Species Difference in Plasma Protein Binding of KE-298 and Its Metabolites
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概要
- 論文の詳細を見る
In vitro protein binding of KE-298 and its plasma metabolites, deacetyl-KE-298(M-1)and S-methyl-KE-298(M-2), was high in rat(>97%), dog(>89%)and human plasma(>99%), respectively. Human serum albumin(>93%)was the main protein involved in the binding to plasma proteins, while the binding to human serum globulins was low(16-33%). The binding of KE-298 and its metabolites in all species of plasma was stereoselective. The(+)-(S)-enantiomers of these compounds bound rat, dog and human plasma proteins to a greater extent than did the(-)-(R)-enantiomers, except that the case of KE-298 was opposite in rat plasma. The stereoselective plasma levels of these compounds in rats, dogs, or humans would likely be due to stereoselective differences in binding to plasma albumin. The protein binding of M-1 in adjuvant-induced arthritis rat plasma was >97%, and the stereoselectivity was similar to the case of normal rat plasma. KE-298 and its metabolites remarkably displaced [^<14>C]warfarin, which bound on albumin in a solution of diluted rat serum albumin. Similarly, there was a displacement of[^<14>C]warfarin in solutions of dog and human serum albumin, and concomitantly the displacement of[^<14>C]diazepam. [^3]H Digitoxin was not displaced by any of the enantiomers in each albumin solution. No stereoselectivity was found in displacement by enantiomers of the three compounds. These results suggest that stereoselective protein binding can be attributed to quantitative differences in binding to albumin rather than to the different binding sites.
- 公益社団法人日本薬学会の論文
- 2001-07-01
著者
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Yoshida Hideo
Department Of Pediatric Surgery Chiba University Graduate School Of Medicine
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Hasegawa Masatoshi
Department Of Drug Metabolism Research Center Taisho Pharmacetutical Co. Ltd.
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Yoshimura Hidetoshi
Faculty Of Pharmaceutical Sciences Kyushu University(present):department Of Food And Nutrition Nakam
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Yoshida H
Lab. Of Food & Nutritional Sciences Dep. Of Nutritional Sci. Kobe-gakuin Univ.
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Yoshimura H
Faculty Of Pharmaceutical Sciences Kyushu University(present):department Of Food And Nutrition Nakam
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ENDO Hiromi
Department of Drug Metabolism, Research Center, Taisho Pharmaceutical Co., Ltd.,
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Higuchi Shohei
Department Of Drug Metabolism Research Center Taisho Pharmacetutical Co. Ltd.
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Endo H
Department Of Drug Metabolism Research Center Taisho Pharmacetutical Co. Ltd.
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OHMI Naoko
Department of Drug Metabolism, Research Center, Taisho Pharmacetutical Co., Ltd.
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HORIUCHI Nobuko
Department of Drug Metabolism, Research Center, Taisho Pharmacetutical Co., Ltd.
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HAMADA Yuka
Department of Pharmacology, Research Center, Taisho Pharmacetutical Co., Ltd.
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Horiuchi Nobuko
Department Of Drug Metabolism Research Center Taisho Pharmacetutical Co. Ltd.
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Ohmi Naoko
Department Of Drug Metabolism Research Center Taisho Pharmacetutical Co. Ltd.
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Hamada Y
Department Of Pharmacology Research Center Taisho Pharmacetutical Co. Ltd.
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Hasegawa Masatoshi
Department Of Chemistry Faculty Of Science Toho University
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Yoshida Hideo
Department Of Aeronautics And Astronautics Kyoto University
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HASEGAWA Masatoshi
Department of Applied Chemistry, Faculty of Science, University of Tokyo
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Endo Hiromi
Department of Chemical Engineering, Faculty of Engineering, Hiroshima University
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吉村 英敏
Department of Nutritional Science, Kobe Gakuin University
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