Dingledine R, Hynes M A, King G L
J Physiol. 1986 Nov;380:175-89. doi: 10.1113/jphysiol.1986.sp016279.
The effects of the N-methyl-D-aspartate (NMDA) receptor antagonist, D-2-amino-5-phosphonovaleric acid (D-APV), and other excitatory amino acid antagonists, were studied on CA1 pyramidal neurones treated with picrotoxin or bicuculline to reduce synaptic inhibition mediated by gamma-aminobutyric acid (GABA). Under these conditions epileptiform burst firing is readily produced by orthodromic stimulation of the pyramidal cell population. D-APV reduced the plateau amplitude and duration of the depolarization underlying evoked and spontaneous bursts without affecting membrane potential, input resistance or the ability of the cell to fire a Ca2+ spike or a short train of Na+ spikes. A late component of the subthreshold excitatory post-synaptic potential (e.p.s.p.) was voltage dependent, being reduced in amplitude on membrane hyperpolarization. D-APV selectively removed this component of the e.p.s.p. in disinhibited slices. In contrast, in the absence of GABA antagonists, D-APV had no noticeable effect on the e.p.s.p. as studied with field potential recordings. The concentration-response relationship of the inhibitory effect of D-APV and L-APV on population spike bursts was studied. The action of APV was highly stereoselective; the EC50 of D-APV was approximately 700 nM, whereas a similar inhibition required 540 microM-L-APV. A number of other excitatory amino acid antagonists were tested at a fixed concentration (100 microM). Among them, the quisqualate antagonist gamma-D-glutamylaminomethyl sulphonic acid was ineffective against epileptiform bursts. In the low nanomolar concentration range both D- and L-APV potentiated bursting. These results suggest that in the absence of GABAergic inhibition, a significant component of the slow depolarization underlying burst firing is voltage dependent, synaptic in origin and mediated by NMDA receptors. We propose that, under normal (non-epileptic) physiological conditions, the balance between synaptic inhibition mediated by GABA receptors and synaptic excitation mediated by NMDA receptors may modulate the excitability of pyramidal cell dendrites.
研究了 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂 D-2-氨基-5-磷酸戊酸(D-APV)及其他兴奋性氨基酸拮抗剂对用印防己毒素或荷包牡丹碱处理以减少γ-氨基丁酸(GABA)介导的突触抑制作用的 CA1 锥体神经元的影响。在这些条件下,通过锥体细胞群的顺向刺激很容易产生癫痫样爆发放电。D-APV 降低了诱发和自发爆发放电所依赖的去极化的平台期幅度和持续时间,而不影响膜电位、输入电阻或细胞产生 Ca2+ 峰电位或短串 Na+ 峰电位的能力。阈下兴奋性突触后电位(e.p.s.p.)的一个晚期成分是电压依赖性的,在膜超极化时幅度减小。D-APV 在去抑制切片中选择性地消除了 e.p.s.p. 的这一成分。相比之下,在没有 GABA 拮抗剂的情况下,用场电位记录研究发现 D-APV 对 e.p.s.p. 没有明显影响。研究了 D-APV 和 L-APV 对群体峰电位爆发抑制作用的浓度-反应关系。APV 的作用具有高度立体选择性;D-APV 的 EC50 约为 700 nM,而类似的抑制作用则需要 540 μM 的 L-APV。在固定浓度(100 μM)下测试了多种其他兴奋性氨基酸拮抗剂。其中,quisqualate 拮抗剂γ-D-谷氨酰胺甲基磺酸对癫痫样爆发放电无效。在低纳摩尔浓度范围内,D-APV 和 L-APV 都增强了爆发放电。这些结果表明,在没有 GABA 能抑制的情况下,爆发放电所依赖的缓慢去极化的一个重要成分是电压依赖性的,起源于突触且由 NMDA 受体介导。我们提出,在正常(非癫痫)生理条件下,GABA 受体介导的突触抑制与 NMDA 受体介导的突触兴奋之间的平衡可能调节锥体细胞树突的兴奋性。