Pharmacological study of TA-0910, a new thyrotropin-releasing hormone(TRH) analog. (I). Effects on the central nervous system by oral administration.
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概要
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Effects of orally administered TA-0910, a new thyrotropin-releasing hormone (TRH) analog, on the central nervous system (CNS) were investigated and compared with those of TRH. TA-0910 shortened the duration of pentobarbital-induced sleep and antagonized reserpine-induced hypothermia at 0.3 mg/kg or more in mice. TA-0910 enhanced the spontaneous motor activity at the higher dose of 30 mg/kg in mice. The drug also activated acute spontaneous EEGs in rabbits at 1 mg/kg. TRH produced these effects at about 100 times higher doses than TA-0910. In antagonizing pentobarbital-induced sleep, the dose ratios of i.v. versus p.o. of TA-0910 and TRH were about 1/10 and 1/100, respectively. The duration of the antagonistic action of TA-0910 on pentobarbital-induced sleep in mice was about 8 times longer than that of TRH when administered orally as well as intraveneously. These potent and long-acting TA-0910 effects on the CNS are discussed in connection with its biotransformation.
- 公益社団法人 日本薬理学会の論文
著者
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Nakagawa Hiroyuki
Department Of Applied Chemistry School Of Science And Engineering Waseda University
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Ishida Ryuichi
Department Of Material-process Engineering And Applied Chemistry For Environment
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MAEDA Kayoko
Department of Biochemistry, Mie University Faculty of Medicine
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Tanaka Takashi
Department Of Central Clinical Laboratory Teikyo University Hospital
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Kinoshita Kiyoshi
Department of Pharmacology, Kyoritsu College of Pharmacy
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MAEDA Kayoko
Department of Pharmacology, Safety Research Laboratory, Tanabe Seiyaku
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YAMAMURA Michio
Department of Pharmacology, Safety Research Laboratory, Tanabe Seiyaku
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Ishida Ryuichi
Department of Pharmacology, Safety Research Laboratory, Tanabe Seiyaku
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