ID JOS-cpb.37.2547
著者:名前 著者:別形式 Kawaguchi, Takeo / Ishikawa, Kozo / Seki, Toshinobu / Juni, Kazuhiko / Fukushima, Shoji / Nakano, Masahiro
著者:カナ 著者:所属 城西大学薬学部 / 城西大学薬学部 / 城西大学薬学部 / 城西大学薬学部 / 熊本大学医学部附属病院 / 熊本大学医学部附属病院
著者:所属(別形式) Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Kumamoto University Hospital, Department of Pharmacy / Kumamoto University Hospital, Department of Pharmacy
著者版フラグ publisher
出版地 東京
出版者 日本薬学会
出版者:カナ ニホンヤクガクカイ
出版者:別名 The Pharmaceutical Society of Japan
NCID AA00602100
冊子ISSN 00092363
電子ISSN 13475223
掲載誌名 巻 37
号 9
刊行年月 1989-09
開始ページ 2547
終了ページ 2549
コンテンツ作成日 1989-02-22
コンテンツ登録日 2014-03-20
識別番号:DOI info:doi/10.1248/cpb.37.2547
識別番号:DOI(リンク) 識別番号:その他 JOI:JST.Journalarchive/cpb1958/37.2547
抄録 N4-Benzoyl-2', 3'-dideoxy-2', 3'-didehydrocytidine (Bz-DDCN) was synthesized as a novel prodrug of 2', 3'-dideoxy-2', 3'-didehydrocytidine (DDCN), which is a reverse transcriptase inhibitor and is considered to be a potential antiacquired immunodeficiency syndrome agent. Chemical and enzymatic regeneration of DDCN from the prodrug has been investigated in both in vitro and in vivo experiments. Bz-DDCN regenerated DDCN under basic conditions (>pH 8), while cleavage of the N-glycosidic linkage and production of N4-benzoylcytosine were observed under acidic conditions (>pH 6). DDCN was enzymatically regenerated from the prodrug in the presence of several enzyme preparations, including human plasma. DDCN and Bz-DDCN were intravenously administered to mice and the plasma concentrations of DDCN and the prodrug were measured. Though DDCN levels following direct DDCN administraiton decreased exponentially with a half-life of 14.5min, the plasma levels of DDCN following the prodrug administration were sustained above 2μM for over 3h.
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