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舒立克隆单剂量效应的睡眠实验室研究。

Sleep laboratory studies on single dose effects of suriclone.

作者信息

Saletu B, Frey R, Grünberger J, Krupka M, Anderer P, Musch B

机构信息

Department of Psychiatry, School of Medicine, University of Vienna, Austria.

出版信息

Br J Clin Pharmacol. 1990 Nov;30(5):703-10. doi: 10.1111/j.1365-2125.1990.tb03839.x.

DOI:10.1111/j.1365-2125.1990.tb03839.x
PMID:1980201
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1368170/
Abstract
  1. In a double-blind, placebo-controlled sleep laboratory study single doses of suriclone, a new non-benzodiazepine anxiolytic binding to benzodiazepine receptors, were investigated with respect to sleep and awakening. 2. Sixteen healthy young volunteers spent 10 nights in the sleep laboratory: 1 adaptation night, 1 baseline night and 4 drug nights (placebo; 0.2 mg, 0.4 mg suriclone; 2 mg lorazepam as reference drug) and 4 subsequent wash-out nights (drug-interval: 1 week). Somnopolygraphic investigations (22.30 h to 06.00 h) were commenced 0.5 h after drug-intake. A self-rating scale for sleep and awakening quality as well as psychometric tests were completed in the morning. 3. Hypnotic effects were most pronounced after lorazepam in regard to total sleep time and sleep efficiency. After lorazepam as well as after 0.4 mg suriclone nocturnal awakenings decreased significantly as compared with placebo, which was reflected in an improved subjective sleep quality after both dosages. Suriclone 0.2 mg did not induce any alterations in all night sleep. 4. In the morning, well-being, drowsiness and reaction time performance deteriorated after lorazepam as compared with placebo but not after suriclone. The latter was significantly superior to lorazepam with respect to subjective awakening quality, well-being, emotional rapport, drowsiness and attention. 5. Blood pressure and pulse remained unchanged after all of the drugs. Critical flicker frequency and muscle strength decreased only after lorazepam as compared with placebo.
摘要
  1. 在一项双盲、安慰剂对照的睡眠实验室研究中,对一种新型非苯二氮䓬类抗焦虑药舒立克隆(suriclone)进行了单剂量研究,该药可与苯二氮䓬受体结合,研究内容涉及睡眠和觉醒情况。2. 16名健康年轻志愿者在睡眠实验室度过10个夜晚:1个适应夜、1个基线夜、4个用药夜(安慰剂;0.2毫克、0.4毫克舒立克隆;2毫克劳拉西泮作为参比药物)以及随后4个洗脱夜(药物间隔:1周)。在服药后0.5小时开始进行睡眠多导描记研究(22:30至06:00)。早晨完成睡眠和觉醒质量自评量表以及心理测试。3. 就总睡眠时间和睡眠效率而言,劳拉西泮的催眠效果最为显著。与安慰剂相比,劳拉西泮以及0.4毫克舒立克隆用药后夜间觉醒次数显著减少,这在两种剂量用药后主观睡眠质量的改善中得到体现。0.2毫克舒立克隆对整夜睡眠未产生任何改变。4. 早晨,与安慰剂相比,劳拉西泮用药后幸福感、嗜睡感和反应时间表现变差,但舒立克隆用药后未出现这种情况。在主观觉醒质量、幸福感、情感融洽度、嗜睡感和注意力方面,舒立克隆明显优于劳拉西泮。5. 所有药物用药后血压和脉搏均保持不变。与安慰剂相比,仅劳拉西泮用药后临界闪烁频率和肌肉力量下降。

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本文引用的文献

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Differences between cyclopyrrolones (suriclone and zopiclone) and benzodiazepine binding to rat hippocampus photolabelled membranes.
Biochem Pharmacol. 1983 Dec 1;32(23):3651-3. doi: 10.1016/0006-2952(83)90318-0.
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Suriclone: a new cyclopyrrolone derivative recognizing receptors labeled by benzodiazepines in rat hippocampus and cerebellum.舒立克隆:一种新型环吡咯酮衍生物,可识别大鼠海马体和小脑中由苯二氮䓬标记的受体。
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Suriclone, a new anxiolytic of the cyclopyrrolone family: evidence for possible interference with GABAergic systems.环吡咯酮类新型抗焦虑药舒立克隆:对γ-氨基丁酸能系统可能存在干扰的证据
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Anxiolytic cyclopyrrolones zopiclone and suriclone bind to a novel site linked allosterically to benzodiazepine receptors.抗焦虑环吡咯酮类药物佐匹克隆和舒里克隆与一个与苯二氮䓬受体变构连接的新位点结合。
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Suriclone and diazepam in the treatment of neurotic anxiety. A double-blind cross-over trial.舒必利克隆与地西泮治疗神经症性焦虑的双盲交叉试验。
Psychopharmacology (Berl). 1987;93(3):296-300. doi: 10.1007/BF00187246.
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Zopiclone. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic.佐匹克隆。对其作为催眠药的药效学、药代动力学特性及治疗效果的综述。
Drugs. 1986 Jul;32(1):48-65. doi: 10.2165/00003495-198632010-00003.