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(4S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl-L-prolinamide, (S)-N-((S)-1-((S)-2-Carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide, (S)-N-[(Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl]-L-histidyl-L-prolinamide, TA 0910, TA-0910, TA0910
C17H23N7O5 · xC2H4O2
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生化/生理作用
Taltirelin (TA-0910) is a thyrotropin-releasing hormone (TRH) mimetic with greatly enhanced brain-penetration, oral activity and stability. Taltirelin shortens the duration of pentobarbital-induced sleep (0.3-3 mg/kg po. or 0.03-0.3 mg/kg iv.), antagonizes reserpine-induced hypothermia (1 or 3 mg/kg po. or 0.1-0.3 mg/kg ip.), and enhances the spontaneous motor activity (30 mg/kg po.) in mice in vivo, while TRH produces these effects at about 100 times higher doses.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
监管及禁止进口产品
Japanese journal of pharmacology, 53(4), 451-461 (1990-08-01)
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
Behavioural brain research, 360, 255-261 (2018-12-12)
Fatigue is a common symptom in many diseases and disorders and can reduce quality of life, yet lacks an adequate pharmacological intervention. To identify and develop such interventions, and to better understand fatigue, additional preclinical research is necessary. However, despite
Frontiers in cellular neuroscience, 12, 485-485 (2019-01-09)
Dopaminergic neurons loss is one of the main pathological characters of Parkinson's disease (PD), while no suitable neuroprotective agents have been in clinical use. Thyrotropin-releasing hormone (TRH) and its analogs protect neurons from ischemia and various cytotoxins, but whether the
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