Liljequist S, Tabakoff B
Life Sci. 1986 Sep 1;39(9):851-5. doi: 10.1016/0024-3205(86)90465-0.
The effect of in vitro addition of pentobarbital to brain membrane preparations from cerebellum and cortex of C57B1 mice was examined in the presence and absence of the specific GABAA receptor "antagonist" bicuculline. In the cortex pentobarbital produced a biphasic effect (stimulation followed by inhibition) on [35S]TBPS binding, whereas only inhibition of [35S]TBPS binding was observed in the cerebellum. When bicuculline was added to assay mixtures, the stimulatory action of pentobarbital was markedly enhanced in the cortex. In the cerebellum the presence of bicuculline uncovered a biphasic effect of pentobarbital on [35S]TBPS binding, that is lower doses of pentobarbital increased, while higher doses decreased [35S]TBPS to the membrane receptors from the cerebellum.
在存在和不存在特异性GABAA受体“拮抗剂”荷包牡丹碱的情况下,研究了体外向C57B1小鼠小脑和皮质的脑膜制剂中添加戊巴比妥的效果。在皮质中,戊巴比妥对[35S]TBPS结合产生双相效应(先刺激后抑制),而在小脑中仅观察到对[35S]TBPS结合的抑制作用。当将荷包牡丹碱添加到测定混合物中时,戊巴比妥在皮质中的刺激作用明显增强。在小脑中,荷包牡丹碱的存在揭示了戊巴比妥对[35S]TBPS结合的双相效应,即较低剂量的戊巴比妥增加,而较高剂量则降低小脑膜受体的[35S]TBPS结合。