Ganong A H, Jones A W, Watkins J C, Cotman C W
J Neurosci. 1986 Apr;6(4):930-7. doi: 10.1523/JNEUROSCI.06-04-00930.1986.
A new series of potent antagonists of excitatory neurotransmission in the rat hippocampus has been identified. These derivatives of piperazine-2,3-dicarboxylate (PzDA) include the most potent acidic amino acid antagonists yet described for Schaffer collateral-commissural EPSPs. These antagonists also effectively block excitatory synaptic responses recorded in the lateral and medial perforant pathways and in the mossy fiber pathway. The PzDA derivatives also block focal depolarizations produced by kainate, quisqualate, and N-methyl-D-aspartate. N-methyl-D-aspartate responses are more susceptible to inhibition by PzDA derivatives, although the spectrum of antagonism of N-methyl-D-aspartate and synaptic responses by PzDA derivatives is not parallel. However, the antagonism of kainate and quisqualate responses by PzDA derivatives shows the same rank order of potency as synaptic responses. These data indicate that synaptic receptors in the hippocampus have a pharmacologic profile similar to that of kainate or quisqualate receptors.
已鉴定出一系列新型强效大鼠海马体兴奋性神经传递拮抗剂。这些哌嗪 - 2,3 - 二羧酸酯（PzDA）衍生物包括迄今为止针对谢弗侧支 - 连合兴奋性突触后电位（EPSP）所描述的最强效酸性氨基酸拮抗剂。这些拮抗剂还能有效阻断在外侧和内侧穿通通路以及苔藓纤维通路中记录到的兴奋性突触反应。PzDA衍生物还能阻断由海藻酸、quisqualate和N - 甲基 - D - 天冬氨酸产生的局灶性去极化。N - 甲基 - D - 天冬氨酸反应更容易受到PzDA衍生物的抑制，尽管PzDA衍生物对N - 甲基 - D - 天冬氨酸和突触反应的拮抗谱并不平行。然而，PzDA衍生物对海藻酸和quisqualate反应的拮抗作用显示出与突触反应相同的效价顺序。这些数据表明，海马体中的突触受体具有与海藻酸或quisqualate受体相似的药理学特征。
