一般薬理 - (株)日本バイオリサーチセンター

Taltirelin hydrate（TA-0910）の一般薬理作用 2.呼吸・循環器系、自律神経系および平滑筋、消化器系、腎機能ならびに体性神経系に対する作用

Taltirelin hydrate（TA-0910）の一般薬理作用 2.呼吸・循環器系、自律神経系および平滑筋、消化器系、腎機能ならびに体性神経系に対する作用.応用薬理,Vol.54(6), 361-381（1997）

Taltirelin hydrate (TA-0910) の一般薬理作用

応用薬理 1997; 54(6): 349-360

Taltirelin hydrate (TA-0910) の一般薬理作用
1. 一般症状および中枢神経系に対する作用
General Pharmacology of Taltirelin hydrate (TA-0910)
1. Effects on Gross Behavior and the Central Nervous System

旭　聡夫¹⁾、山口　和政²⁾、加藤　正巳²⁾、木下　潔¹⁾、山村　道夫¹⁾、松岡　雄三¹⁾1)田辺製薬株式会社　医薬開発研究所
2)株式会社日本バイオリサーチセンター　羽島研究所

Taltirelin hydrate, (-)-N-[(S)-hexahydro-1-methyl-2, 6-dioxo-4-pyrimidinylcarbonyl]-L-histidyl- L-prolinamide tetrahydrate (TA-0910), is an orally active thyrotropin-releasing hormone (TRH) analog. Effects of TA-0910 on gross behavior and the central nervous system (CNS) were investigated using mice, rats, rabbits and dogs. In mice, oral administration of TA-0910 produced hyperlocomotion and tail elevation, and increased preening and grooming behaviors at 10 mg/kg or more. It also produced blinking and eyelid closure at 30 mg/kg or more, and caused salivation, piloerection, tremor, and an increase in respiratory rate at 100 mg/kg. In rats, oral administration of TA-0910 increased rearing, grooming and preening behaviors at 10 mg/kg or more, produced hyperlocomotion and wet-dog shakes at 30 mg/kg or more, and caused eyelid closure at 100 mg/kg. Similar signs were observed in mice and rats administered i.v. with 1 to 10 mg/kg of TRH. TA-0910 increased spontaneous locomotor activity of mice, and raised body temperature of rabbits and arousal stage of spontaneous EEG of dogs at 10 to 30 mg/kg p.o. and at 0.3 to 1 mg/kg i.v. However, it did not affect motor coordination, muscle tone, pain response, pentetrazol- or electroshock-induced convulsion in mice up to 30 mg/kg p.o. and up to 3 mg/kg i.v. TRH produced analgesia in mice and raised body temperature in rabbits at 10 or 30 mg/kg i.v. In conclusion, TA-0910 affected gross behavior and body temperature of rodents at doses of 10 to 100 times its pharmacologically CNS-activating doses (0.3 mg/kg p.o. and 0.03 mg/kg i.v.). These effects were similar to those of TRH. TA-0910 also increased wakefulness of dogs. Except for these effects, TA-0910 exhibited no notable effects in tests for the CNS investigated.

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