SanMartin S, Andrés-Trelles F, Menendez L, Meana A, Hidalgo A, Baamonde A
Laboratorio de Farmacologia, Facultad de Medicina, Oviedo, Spain.
Cell Mol Neurobiol. 1996 Jun;16(3):427-31. doi: 10.1007/BF02088108.
GABAA agonists do not respond to the same degree to allosteric modulators of the GABAA receptor complex such as benzodiazepines. We report there the effects of two steroids (alfaxalone and pregnenolone sulfate) on the inhibition induced by two GABAA agonists, 3-amino propane sulphonic acid (3-APS) and muscimol, on the extracellular evoked potentials obtained in CA1 of mice hippocampi. Alfaxalone (1 microM) potentiates the effects of both agonists, although incubation times longer than 15 minutes are required to potentiate the inhibitory effect of muscimol. Lower doses of pregnenolone sulfate at shorter incubation periods are able to inhibit the effects produced by single doses of 3-APS as compared to muscimol (15 microM during 5 min vs 30 microM during 5 min). Our results confirm the possibility that there might be differences in the interaction between GABAA agonists and modulatory steroids.
GABAA 激动剂对 GABAA 受体复合物的变构调节剂(如苯二氮䓬类药物)的反应程度不尽相同。我们在文中报告了两种甾体化合物(阿法沙龙和硫酸孕烯醇酮)对两种 GABAA 激动剂(3-氨基丙烷磺酸(3-APS)和蝇蕈醇)诱导的抑制作用的影响,这两种激动剂作用于小鼠海马体 CA1 区的细胞外诱发电位。阿法沙龙(1 microM)增强了两种激动剂的作用,不过增强蝇蕈醇的抑制作用需要超过 15 分钟的孵育时间。与蝇蕈醇相比(5 分钟内 15 microM 与 5 分钟内 30 microM),较短孵育时间下较低剂量的硫酸孕烯醇酮能够抑制单剂量 3-APS 产生的作用。我们的结果证实了 GABAA 激动剂与调节性甾体化合物之间的相互作用可能存在差异的可能性。