Yamamoto M, Shimizu M
Department of Pharmacology, Yamanouchi Pharmaceutical Co. Ltd., Tokyo, Japan.
Naunyn Schmiedebergs Arch Pharmacol. 1988 Sep;338(3):262-7. doi: 10.1007/BF00173398.
Effects of a new TRH analogue, YM-14673 (N alpha-[[(S)-4-oxo-2-azetidinyl]carbonyl]-L-histidyl-L-prolinamide dihydrate) on cognitive disturbance of passive avoidance response were studied in rodents in comparison with those of TRH and CDP-choline. The latency for entering from the illuminated into the dark compartments was shortened in anoxia and scopolamine-treated rats, cycloheximide-treated mice and cerebral ischemic gerbils. The shortened latency in these models was prolonged by administration of both YM-14673 and TRH in doses without effect on spontaneous movement. YM-14673 was about 10 times more potent than TRH in ameliorating the cognitive disturbance, whereas CDP-choline showed no influence on the learning ability. These results suggest that YM-14673 and TRH possess facilitatory effects on cerebral function and that YM-14673 was distinct from CDP-choline in pharmacological profile.
将一种新的促甲状腺激素释放激素（TRH）类似物YM - 14673（Nα - [[(S) - 4 - 氧代 - 2 - 氮杂环丁烷基]羰基] - L - 组氨酰 - L - 脯氨酰胺二水合物）与TRH和胞磷胆碱相比，研究其对啮齿动物被动回避反应认知障碍的影响。在缺氧和东莨菪碱处理的大鼠、环己酰亚胺处理的小鼠以及脑缺血沙土鼠中，从光照区进入黑暗区的潜伏期缩短。在这些模型中，给予对自发活动无影响剂量的YM - 14673和TRH后，缩短的潜伏期延长。在改善认知障碍方面，YM - 14673的效力约为TRH的10倍，而胞磷胆碱对学习能力无影响。这些结果表明，YM - 14673和TRH对脑功能具有促进作用，且YM - 14673在药理学特征上与胞磷胆碱不同。
