Little H J, Andreasen M, Lambert J D
Department of Pharmacology, Medical School, Bristol, U.K.
Brain Res. 1992 Feb 28;573(2):243-50. doi: 10.1016/0006-8993(92)90769-6.
We have shown previously that chronic treatment of mice with a benzodiazepine agonist, flurazepam, increased the pharmacological actions of the partial inverse agonist, FG7142. We have investigated the neurophysiological basis for this using extracellular recordings of evoked field potentials in area CA1 of isolated hippocampal slices. The slices were prepared 48 h after the end of the chronic in vivo treatment, a time when no evidence of residual benzodiazepine agonist activity was found in the CNS. During perfusion with standard Ringer solution, no significant differences were seen between the field potentials in slices from flurazepam-treated mice and those from control animals. When FG7142 was added to the perfusion medium there was an increase in the secondary discharges that followed the initial population spikes, and an increase in paired pulse potentiation. These increases were significantly greater in slices from flurazepam-treated mice, compared with controls. The results show that the effects of the partial inverse agonist, FG7142, on an isolated neuronal preparation, were increased by chronic administration of a benzodiazepine agonist in vivo. This effect is suggested to be due to a decrease in GABAergic inhibition.
我们之前已经表明,用苯二氮䓬激动剂氟西泮对小鼠进行长期治疗,会增强部分反向激动剂FG7142的药理作用。我们使用分离的海马切片CA1区诱发场电位的细胞外记录,研究了其神经生理学基础。切片在长期体内治疗结束后48小时制备,此时在中枢神经系统中未发现残留苯二氮䓬激动剂活性的证据。在用标准林格溶液灌注期间,氟西泮治疗小鼠的切片与对照动物的切片的场电位之间未观察到显著差异。当将FG7142添加到灌注介质中时,初始群体峰电位之后的继发性放电增加,成对脉冲增强增加。与对照组相比,氟西泮治疗小鼠的切片中的这些增加显著更大。结果表明,体内长期给予苯二氮䓬激动剂会增强部分反向激动剂FG7142对分离的神经元制剂的作用。这种作用被认为是由于GABA能抑制作用的降低。