Central Nervous System Depressant Effects of N^3-Substituted Derivatives of Deoxyuridine in Mice
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概要
- 論文の詳細を見る
N^3-Substituted derivatives of deoxyuridine (1) were synthesized and their pharmacological effects were evaluated by intracerebroventricular (i.c.v.) injection in mice. Eleven derivatives, including the methyl (2), ethyl (3), propyl (4), allyl (5), butyl (6), benzyl (7), o, m and p-xylyls (8,9,10), α-phenylethyl (11) and phenacyl (12) derivatives, of 1 were prepared and their pharmacological effects were evaluated by using hypnotic activity, pentobarbital-induced sleep prolongation, spontaneous activity and motor incoordination as indices of central nervous system (CNS) depressant effects. At a dose of 2.0 μmol/mouse, the values of mean sleeping time induced by 7,8,9 and 10 were 23,35,29 and 30 min, respectively. Although the alkyl (2-6) derivatives did not cause any hypnotic activity, some derivatives tested (3,5,6,8-12) significantly prolonged the pentobarbital-induced sleeping time. When the CNS depressant effects of phenacyl substituted 1 were compared to that of other oxopyrimidine nucleosides, N^3-phenacyluridine (13), N^3-phenacylthymidine (14), N^3-phenacyl-6-azauridine (15), compounds 12,13 and 14 (1.0 μmol/mouse, i.c.v.) significantly decreased mouse spontaneous activity. Furthermore, 12-15 (1.0 μmol/mouse, i.c.v.) caused mouse motor incoordination. These results indicate that deoxyuridine derivatives have generally central depressant activity, and the benzyl and xylyl derivatives, but not alkyl derivatives, possess hypnotic activity.
- 公益社団法人日本薬学会の論文
- 1996-01-15
著者
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景山 節
京大・霊長類研・生化学
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Yamamoto Ikuo
Department Of Hygienic Chemistry School Of Pharmaceutical Sciences Kyushu University Of Health And W
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Yamamoto Ikuo
Faculty of Education, Yokohama National University
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Kondo Shigemi
Nissui Pharmaceutical Co. Ltd.
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WATANABE Kazuhito
Faculty of Pharmaceutical Sciences, Hokuriku University
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KIMURA Toshiyuki
Faculty of Pharmaceutical Sciences, Hokuriku University
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HO Ing
University of Mississippi Medical Center
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舘岡 裕二
Shinshin Chemical Industry Co. Ltd.
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Yamamoto Ikuo
北陸大学 薬 衛化
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YAMAMOTO IKUO
Hygienic Chemistry
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Kimura T
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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景山 節
京都大学霊長類研究所人類進化モデル研究センター
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景山 節
京大・霊長研
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Ho Ing
ミシシッピ大学医学部薬毒理学教室
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Watanabe Kazuhito
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Kimura T
Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe
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Kimura Toshiyuki
Faculty Of Engineering Yokohama National University
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Kondo S
Kyoritsu Coll. Pharmacy Tokyo Jpn
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Tateoka Yuji
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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KUZE Jiro
Faculty of Pharmaceutical Sciences, Hokuriku University
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TERAOKA Seisaku
Faculty of Pharmaceutical Sciences, Hokuriku University
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TATEOKA Yuji
Shinshin Chemical Industries, Ltd.
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HO IngKang
University of Mississippi Medical Center
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Kuze J
Faculty Of Pharmaceutical Sciences Hokuriku University
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Teraoka Seisaku
Faculty Of Pharmaceutical Sciences Hokuriku University
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Watanabe Kazuhito
Faculty Of Pharmaceutical Sciences Hokuriku University
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Yamamoto I
Hygienic Chemistry
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Watanabe Kazuhito
Faculty Of Pharmaceutical Sciences Kyushu University
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Yamamoto Ikuo
Faculty Of Education Yokohama National University
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Kimura T
Peptide Inst. Inc. Minoh Jpn
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