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咯利普兰是一种可提高环磷酸腺苷可用性的抗抑郁药,它能短暂增强大鼠的清醒程度。

Rolipram, an antidepressant that increases the availability of cAMP, transiently enhances wakefulness in rats.

作者信息

Lelkes Z, Alföldi P, Erdos A, Benedek G

机构信息

Department of Physiology, Albert Szent-Györgyi Medical University, Szeged, Hungary.

出版信息

Pharmacol Biochem Behav. 1998 Aug;60(4):835-9. doi: 10.1016/s0091-3057(98)00038-0.

DOI:10.1016/s0091-3057(98)00038-0
PMID:9700966
Abstract

A study was carried out on the effects on sleep of rolipram, an antidepressant that increases the availability of cAMP by inhibiting a phosphodiesterase isoenzyme. Rats were treated with rolipram (0.1 or 1 mg/kg) twice a day (at light and dark onset) for 11 days, after a chronic period of injection of physiological saline for habituation purposes. The sleep-wake activity was recorded for 12 h following the injection at light onset on the baseline day (physiological saline), on rolipram days 1, 5, and 11, and also on day 12, when physiological saline was injected again (withdrawal day). The high (1 mg/kg) dose of rolipram enhanced wakefulness (W) in postinjection h 1 on day 1 of rolipram treatment. After administration of 0.1 mg/kg rolipram, only a tendency to an increase in W was noted. The promotion of W might be attributed, at least in part, to an increased release of noradrenaline due to a cAMP-mediated stimulation of tyrosine hydroxylase.

摘要

一项关于咯利普兰(一种通过抑制磷酸二酯酶同工酶来提高环磷酸腺苷可用性的抗抑郁药)对睡眠影响的研究展开。为了适应环境,大鼠先经过一段慢性注射生理盐水的时期,之后每天两次(在光照和黑暗开始时)用咯利普兰(0.1或1毫克/千克)进行处理,持续11天。在基线日(注射生理盐水)、咯利普兰处理的第1天、第5天和第11天以及再次注射生理盐水的第12天(撤药日),在光照开始时注射后记录12小时的睡眠-觉醒活动。高剂量(1毫克/千克)的咯利普兰在咯利普兰处理第1天注射后第1小时增强了觉醒(W)。给予0.1毫克/千克咯利普兰后,仅观察到W有增加的趋势。W的增加至少部分可归因于环磷酸腺苷介导的酪氨酸羟化酶刺激导致去甲肾上腺素释放增加。

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