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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Positive allosteric modulation of mGlu7 receptors by AMN082 affects sleep and wakefulness in the rat
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Positive allosteric modulation of mGlu7 receptors by AMN082 affects sleep and wakefulness in the rat

机译：AMN082对MGLU7受体的积极构建调节影响大鼠的睡眠和清醒

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Evidence indicates that metabotropic glutamate receptors (mGlu) are involved in the regulation of physiological and behavioral processes, and glutamate has been implicated in several pathologies of the Central Nervous System. Pharmacological evidence suggests the therapeutic potential of targeting mGlu7 receptor in a number of pathological conditions; and previous research has shown the involvement of glutamate on sleep and wakefulness regulation. Here, the effects of mGlu7 receptor selective modulation on sleep and wake states are explored. 32 male Wistar rats were implanted with electrodes for recording sleep and wakefulness. N,N??-Bis(diphenylmethyl)-1,2- ethanediamine dihydrochloride (AMN082) (5, 10, and 20 mg/kg, i.p.), a potent, selective and systemically active mGlu7 receptor positive allosteric modulator, or vehicle was administered 1 hour after the beginning of the light period. AMN082 (5 and 10 mg/kg) significantly increased total time of sleep; and time spent on Slow Wave Sleep (SWS) was increased. AMN082 at 10 mg/kg specifically affected Light SWS, increasing time spent on Light SWS. The highest dose of AMN082, 20 mg/kg, significantly reduced time spent in Rapid Eye Movement (REM) sleep, decreasing the number of REM sleep episodes and their mean duration. Total time spent awake was increased and mean episode duration of wakefulness was prolonged. The present results suggest that mGlu7 receptors might be involved in sleep regulation and drugs targeting these receptors could affect sleep and wakefulness architecture. ? 2012 Elsevier Inc.
机译：证据表明，代谢谷氨酸受体（MGLU）参与了生理和行为过程的调节，并且谷氨酸族在中枢神经系统的几种病理中涉及。药理证据表明在许多病理条件下靶向MGLU7受体的治疗潜力;先前的研究表明，谷氨酸对睡眠和清醒调节的参与。这里，探讨了MGLU7受体选择性调节对睡眠和唤醒状态的影响。将32只雄性Wistar大鼠植入电极以记录睡眠和清醒。 N，N ?? - 双（二苯基甲基）-1,2-乙二胺二盐（AMN082）（5,10和20mg / kg，IP），有效的，选择性和系统性的MGLU7受体阳性变构调制剂或载体是在光周期开始后1小时施用。 AM082（5和10 mg / kg）显着增加睡眠时间;并且在慢波睡眠（SWS）上花了时间。 AM082以10毫克/公斤特异性影响光线SWS，越来越多的时间在轻型速度下花了。 AM082，20mg / kg的最高剂量显着降低了在快速眼运动（REM）睡眠中花费的时间，降低了REM睡眠剧集的数量及其平均持续时间。唤醒的总时间提高，延长了醒来的觉醒的季节性持续时间。本结果表明，MGLU7受体可能参与睡眠调节，靶向这些受体可能会影响睡眠和醒来的架构。还2012年elsevier公司

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