Lancel M, Faulhaber J
Max-Planck Institute of Psychiatry, Department of Neuroendocrinology, Munich, Germany.
Neuroreport. 1996 Sep 2;7(13):2241-5. doi: 10.1097/00001756-199609020-00036.
To investigate the effects of the selective gamma-aminobutyric acid (GABA)A receptor agonist 4,5,6,7-tetrahydroisoxazolo (5,4-c)pyridin-3-ol (THIP) on sleep, vehicle or 2 or 4 mg kg-1 of THIP were randomly administered i.p. to 8 rats at light onset. EEG and EMG were recorded during the first 6 hours after injection. THIP 4 mg kg-1 transiently evoked bursts of absence epilepsy-like EEG hypersynchronization. It significantly promoted non-rapid eye movement (non-REM) sleep and elevated delta activity within non-REM sleep. This was accompanied by an increase in both the rise rate and maximal level of delta activity within the non-REM sleep episodes. The effects of THIP on sleep resemble those reported earlier for the GABAA agonist muscimol and are dissimilar from those induced by benzodiazepine-agonistic modulators of GABAA receptors. These data indicate that agonists and agonistic modulators of GABAA receptors affect sleep differentially.
为研究选择性γ-氨基丁酸（GABA）A受体激动剂4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇（THIP）对睡眠的影响，在光照开始时将溶剂或2或4mg/kg的THIP腹腔注射给8只大鼠。在注射后的前6小时记录脑电图（EEG）和肌电图（EMG）。4mg/kg的THIP短暂诱发失神癫痫样脑电图超同步爆发。它显著促进非快速眼动（non-REM）睡眠并提高非快速眼动睡眠中的δ波活动。这伴随着非快速眼动睡眠期间δ波活动的上升速率和最大水平的增加。THIP对睡眠的影响类似于先前报道的GABAA激动剂蝇蕈醇的影响，并且与GABAA受体的苯二氮卓激动剂调节剂诱导的影响不同。这些数据表明GABAA受体激动剂和激动剂调节剂对睡眠的影响不同。
