Pharmacological study of TA-0910, a new thyrotropin-releasing hormone (TRH) analog, (I): Effects on the central nervous system by oral administration

Japanese Journal of Pharmacology
M YamamuraR Ishida

Abstract

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 intravenously. These potent and long-acting TA-0910 effects on the CNS are discussed in connection with its biotransformation.

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Citations

May 7, 1998·European Journal of Pharmacology·K KinoshitaY Matsuoka
Jul 6, 2015·European Journal of Pharmacology·Tomoyuki IjiroHitoshi Ishibashi
Nov 3, 2011·Journal of Receptor and Signal Transduction Research·Hidetoshi AsaiOsamu Doi
Jan 5, 2000·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·F YonemoriA Tamura
Apr 1, 1992·Alcoholism, Clinical and Experimental Research·A H RezvaniG A Mason
Nov 13, 2019·Journal of Peptide Science : an Official Publication of the European Peptide Society·Naotake KobayashiTakayoshi Yoshikawa
May 28, 2020·Frontiers in Pharmacology·Jean-Louis CharliPatricia Joseph-Bravo
Feb 1, 2011·Journal of Medicinal Chemistry·Phuc Ung, David A Winkler

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