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腺苷 A 2A 受体激动剂 CGS21680 模拟前列腺素 D2 诱发大鼠生理性睡眠
引用本文:刘炜,黄志力,曲卫敏. 腺苷 A 2A 受体激动剂 CGS21680 模拟前列腺素 D2 诱发大鼠生理性睡眠[J]. 中国药学杂志, 2009, 44(23): 1786-1790
作者姓名:刘炜  黄志力  曲卫敏
摘    要: 目的 内源性前列腺素( prostaglandin, PG ) D2 能增加基底前脑下蛛网膜下腔内的腺苷水平,可能作用于腺苷 A 2A 受体,诱发睡眠。本实验观察腺苷 A 2A 受体特异性激动剂 CGS21680 和 PGD2 促眠作用的异同。 方法 手术插入不锈钢导管至大鼠基底前脑下蛛网膜下腔,同时埋植脑电波和肌电波记录电极,术后 2 周,经导管微量恒速灌注 PGD2 ( 200 pmol·0.2 μL-1·min-1 )或 CGS21680 ( 10 pmol·0.2 μL-1·min-1 ),同步记录脑电波和肌电波,分析睡眠量、睡眠强度及睡眠时相转换等参数。 结果 与人工脑脊液自身对照相比, PGD2 和 CGS21680 都显著增加慢波睡眠(非快动眼睡眠)量和睡眠强度,两者在时相转化和各波段时程上表现出高度的相似性。 CGS21680 增加快动眼睡眠量,而 PGD2 不引起快动眼睡眠量的增加。 结论 ■ 腺苷 A 2A 受体激动剂 CGS21680 能模拟 PGD2 诱发的慢波睡眠,提示腺苷 A 2A 受体是诱导生理性睡眠的重要靶点之一。

关 键 词:腺苷 A 2A 受体  CGS21680  脑电图  前列腺素 D2  大鼠  睡眠
收稿时间:2000-01-01;

An Adenosine A 2A Receptor Agonist CGS21680 Mimic s Prostaglandin D2 to Induce Physiological Sleep in Rats
LIU W ei,HUANG Z hi- l i,QU W ei- m in. An Adenosine A 2A Receptor Agonist CGS21680 Mimic s Prostaglandin D2 to Induce Physiological Sleep in Rats[J]. Chinese Pharmaceutical Journal, 2009, 44(23): 1786-1790
Authors:LIU W ei  HUANG Z hi- l i  QU W ei- m in
Affiliation:( Shanghai Medical College of Fudan University, a. State Key Laboratory of Medical Neurobiology; b . Department of Pharmacology , Shanghai 200032, China
Abstract:OBJECTIVE To compare the sleep-wake profiles induced by endogenous prostaglandin (PG)D2 and CGS21680, an adenosine A2A receptor agonist. METHODS Under 10% chloral hydrate anesthesia [360 mg·kg-1 intraperitoneal (i.p.)], rats underwent the surgery for implantation of electrodes for electroencephalogram (EEG) and electromyogram recordings and placement of a stainless steel cannula inserted stereotaxically into the subarachnoid space under the basal forebrain for infusion of PGD2 or CGS21680. The software SleepSign was used to analyze EEG parameters, including sleep amount, sleep episode, stage transition and power density. RESULTS PGD2 and CGS21680 induced non-rapid eye movement sleep was similar to physiological sleep with the same amounts, identical patterns of sleep episode number and duration, stage transition, and power density. CONCLUSION Activation of adenosine A2A receptors by CGS21680 mimicked the somnogenic effects of PGD2.
Keywords:adenosine A2A receptor  CGS21680  electroencephalogram  prostaglandin D2  rat  sleep
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