Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia.
Yerkes National Primate Research Center, Emory University, Atlanta, Georgia.
J Neurosci Res. 2018 Jul;96(7):1324-1335. doi: 10.1002/jnr.24230. Epub 2018 Mar 25.
N-methyl-D-aspartate receptors (NMDARs) are ion channels comprising tetrameric assemblies of GluN1 and GluN2 receptor subunits that mediate excitatory neurotransmission in the central nervous system. Of the four different GluN2 subunits, the GluN2D subunit-containing NMDARs have been suggested as a target for antiparkinsonian therapy because of their expression pattern in some of the basal ganglia nuclei that show abnormal firing patterns in the parkinsonian state, specifically the subthalamic nucleus (STN). In this study, we demonstrate that blockade of NMDARs altered spike firing in the STN in a male nonhuman primate that had been rendered parkinsonian by treatment with the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. In accompanying experiments in male rodents, we found that GluN2D-NMDAR expression in the STN was reduced in acutely or chronically dopamine-depleted animals. Taken together, our data suggest that blockade of NMDARs in the STN may be a viable antiparkinsonian strategy, but that the ultimate success of this approach may be complicated by parkinsonism-associated changes in NMDAR expression in the STN.
N-甲基-D-天冬氨酸受体(NMDAR)是由 GluN1 和 GluN2 受体亚基组成的四聚体离子通道,在中枢神经系统中介导兴奋性神经传递。在四种不同的 GluN2 亚基中,含有 GluN2D 亚基的 NMDAR 被认为是抗帕金森病治疗的靶点,因为它们在一些基底神经节核中表达,这些核在帕金森病状态下表现出异常的放电模式,特别是丘脑底核(STN)。在这项研究中,我们证明了在雄性非人类灵长类动物中,用神经毒素 1-甲基-4-苯基-1,2,3,6-四氢吡啶处理使其帕金森病后,阻断 NMDAR 会改变 STN 中的尖峰放电。在雄性啮齿动物的伴随实验中,我们发现急性或慢性多巴胺耗竭动物的 STN 中 GluN2D-NMDAR 表达减少。总之,我们的数据表明,阻断 STN 中的 NMDAR 可能是一种可行的抗帕金森病策略,但由于帕金森病相关的 STN 中 NMDAR 表达的变化,这种方法的最终成功可能会变得复杂。