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褪黑素激动剂S-20098对大鼠昼夜活动节律重新调整方向的剂量依赖性效应。

Dose dependent effects of S-20098, a melatonin agonist, on direction of re-entrainment of rat circadian activity rhythms.

作者信息

Redman J R, Guardiola-Lemaitre B, Brown M, Delagrange P, Armstrong S M

机构信息

Department of Psychology, Monash University, Clayton, Victoria, Australia.

出版信息

Psychopharmacology (Berl). 1995 Apr;118(4):385-90. doi: 10.1007/BF02245938.

DOI:10.1007/BF02245938
PMID:7568624
Abstract

The chronobiotic properties of melatonin are well documented. For example, following an 8-h phase advance of the light-dark cycle daily injections of melatonin administered at the pre-shift dark onset alter the direction of re-entrainment of rat activity rhythms. Using this 8-h phase advance paradigm, the effects of the melatonin agonist S-20098 (1 mg/kg and 3 mg/kg) on the rat circadian system were compared with those of melatonin. S-20098 altered the direction of re-entrainment in the same manner as melatonin. A study using lower doses of S-20098 showed that the effect on direction of re-entrainment was dose-dependent, with 100% of rats responding at a dose of 100 micrograms/kg. S-20098 may, therefore, have therapeutic potential as a chronobiotic in the treatment of circadian disorders in humans.

摘要

褪黑素的生物钟调节特性已有充分记载。例如,在明暗周期提前8小时的情况下,每天在提前转变的黑暗开始时注射褪黑素,会改变大鼠活动节律的重新同步方向。利用这种提前8小时的相位提前模式,将褪黑素激动剂S-20098(1毫克/千克和3毫克/千克)对大鼠昼夜节律系统的影响与褪黑素的影响进行了比较。S-20098与褪黑素以相同方式改变重新同步方向。一项使用较低剂量S-20098的研究表明,对重新同步方向的影响呈剂量依赖性,100微克/千克剂量时100%的大鼠有反应。因此,S-20098作为一种生物钟调节药物在治疗人类昼夜节律紊乱方面可能具有治疗潜力。

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