Examination of Local Anti-inflammatory Activities of New Steroids, Hemisuccinyl Methyl Glycolates
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概要
- 論文の詳細を見る
To overcome the side effects of steroids, novel steroid-17-yl methyl glycolates with succinyl group at C-20,derived from predinisolone and dexamethasone were prepared based on concept of the antedrug. Their topical anti-inflammatory activity and systemic effects were evaluated trough croton oil-induced ear edema and paper disk granuloma bioassay. Among them, (20S)-succinyl dexamethasone derivatives (7 and 11) indicated more potent ati-inflammatory activity than the parent dexamethasone and did not show corticosteroidal side effects of thymic, adrenal involution or body weight loss. Both 7 and 11 were immediately metabolized into active compound 3 and this metabolite was eliminated with mean half-lives of 0.786 to 0.866 h in rat serum. Our findings suggest that these two compounds might be candidates as the novel steroids, and that that introduction of the succinyl group into the methyl glycolates at C-20 is useful to avoid suppressiion of organs due to the side effects of corticosteroids.
- 公益社団法人日本薬学会の論文
- 1999-08-15
著者
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斎藤 徹
Faculty Of Pharmaceutical Sciences Kanazawa University
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SUZUKI Toshio
Department of Animal Science, Faculty of Agriculture, Utsunomiya University
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Sato E
Department Of Pharmaceutical Science Akita University School Of Medicine
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Suzuki T
Drug Discovery Research Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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TADA Hitoshi
Department of Pharmaceutical Science, Akita University Hospital
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鈴木 徳治
千葉大 薬
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Suzuki T
Laboratory Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Chiba University
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Saito T
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Saito Takako
Research And Development Laboratories Maruho Co. Ltd.
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SATO ETSUKO
Department of Pharmaceutical Science, Akita University School of Medicine
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TOJIMA Yoichi
Ohta Pharmaceutical Co., Ltd.,
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Sato Etsuko
Department Of Pharmaceutical Science Akita University School Of Medicine
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Suzuki Toshikazu
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Tojima Yoichi
Ohta Pharmaceutical Co. Ltd.
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Tada H
Department Of Pharmaceutical Science Akita University School Of Medicine
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Tada Hitoshi
Department Of Pharmaceutical Science Akita University Hospital
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Suzuki T
Research Unit Of Pharmaceutics College Of Pharmacy Nihon University
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Sato Etsuko
Department Of Ophthalmology Japanese Red Cross Nagoya First Hospital
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Sugihara T
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Saito T
Research And Development Laboratories Maruho Co. Ltd.
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Suzuki Toshio
Department Of Agronomy Faculty Of Agriculture Tohoku University
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