大鼠发情周期中γ-氨基丁酸A型（GABAA）受体刺激的功能变化
Functional changes in GABAA receptor stimulation during the oestrous cycle of the rat.
作者信息
Westerling P, Lindgren S, Meyerson B
机构信息
Department of Medical Pharmacology, University of Uppsala, Sweden.
出版信息
Br J Pharmacol. 1991 Jun;103(2):1580-4. doi: 10.1111/j.1476-5381.1991.tb09830.x.
Abstract
- Slices of rat cuneate nucleus were used to study whether or not gonadal steroids influence the gamma-aminobutyric acid (GABA) system in vivo. Females in different stages of the oestrous cycle as well as steroid-treated (oestrogen, progesterone or both) ovariectomized animals were used. 2. Functional changes in the GABAA receptors were assayed using the effects of potentiators (benzodiazepine, barbiturate) and antagonists (picrotoxin) on the muscimol control dose-response curves. 3. The potentiating effect of the benzodiazepine, flurazepam was unchanged during the oestrous cycle, and the hormone treatments did not alter this effect. 4. During oestrus, an increase was seen in the potentiating effect of the barbiturate (pentobarbitone). This suggests a synergistic effect between barbiturates and gonadal steroids. Progesterone treatment also increased the effect of pentobarbitone. 5. The antagonistic action of picrotoxin was unaffected during the oestrous cycle. However, progesterone (or progesterone and oestrogen) treatment reduced the potency of picrotoxin. 6. This study supports the idea that endogenous steroids (presumably progesterone) affect the GABAA receptors during the oestrous cycle by a mechanism associated with the barbiturate site of the GABAA receptor complex.
摘要
- 采用大鼠楔束核切片研究性腺类固醇激素是否在体内影响γ-氨基丁酸（GABA）系统。使用处于发情周期不同阶段的雌性大鼠以及经类固醇激素处理（雌激素、孕激素或两者皆用）的去卵巢动物。2. 使用增强剂（苯二氮䓬、巴比妥酸盐）和拮抗剂（印防己毒素）对蝇蕈醇对照剂量-反应曲线的影响来测定GABAA受体的功能变化。3. 苯二氮䓬氟西泮的增强作用在发情周期中未发生变化，激素处理也未改变这种作用。4. 在发情期，巴比妥酸盐（戊巴比妥）的增强作用增强。这表明巴比妥酸盐与性腺类固醇激素之间存在协同作用。孕激素处理也增强了戊巴比妥的作用。5. 印防己毒素的拮抗作用在发情周期中未受影响。然而，孕激素（或孕激素与雌激素）处理降低了印防己毒素的效力。6. 本研究支持以下观点：内源性类固醇激素（可能是孕激素）在发情周期中通过与GABAA受体复合物的巴比妥酸盐位点相关的机制影响GABAA受体。
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