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喹哌嗪的睡眠抑制作用:与中枢5-羟色胺能刺激的关系。

Sleep suppressant action of quipazine: relation to central serotonergic stimulation.

作者信息

Fornal C, Radulovacki M

出版信息

Pharmacol Biochem Behav. 1981 Dec;15(6):937-44. doi: 10.1016/0091-3057(81)90058-7.

Abstract

Administration of quipazine maleate (1-10 mg/kg, IP), a proposed 5-hydroxytryptamine (5-HT) receptor stimulant to rats produced a dose-related suppression of both slow-wave sleep (SWS) and rapid-eye-movement sleep (REMS) accompanied by an increase in head-shaking behavior. These effects were observed during the first 6 hr of a 12-hr EEG recording session. The latencies to the sleep states were markedly prolonged and correlated with the duration of head-shaking behavior induced by the drug. A significant inverse relationship was found between the amount of SWS or REMS and the number of head-shakes occurring during the first 6-hr period. Since head-shaking behavior in rodents has been proposed as a quantitative, behavioral model of central 5-HT activation, the data suggest a causal relationship between enhanced 5-HT activity and sleep suppression. This assumption is further supported by the observation that pretreatment with metergoline (2.5 mg/kg, IP) a 5-HT receptor blocker, reduced quipazine's effects on both SWS and head-shaking behavior.

摘要

给大鼠腹腔注射马来酸喹哌嗪(1 - 10毫克/千克),一种假定的5 - 羟色胺(5 - HT)受体兴奋剂,会产生与剂量相关的慢波睡眠(SWS)和快速眼动睡眠(REMS)抑制,同时伴有摇头行为增加。这些效应在12小时脑电图记录期的前6小时观察到。睡眠状态的潜伏期明显延长,且与药物诱发的摇头行为持续时间相关。在前6小时内,慢波睡眠或快速眼动睡眠量与摇头次数之间存在显著的负相关。由于啮齿动物的摇头行为已被提议作为中枢5 - HT激活的定量行为模型,这些数据表明5 - HT活性增强与睡眠抑制之间存在因果关系。5 - HT受体阻滞剂美替拉酮(2.5毫克/千克,腹腔注射)预处理可降低喹哌嗪对慢波睡眠和摇头行为的影响,这一观察结果进一步支持了这一假设。

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