Department of Pharmacology and Pharmacotherapy, Semmelweis University, H-1089 Budapest, Hungary.
Institute of Translational Medicine, Semmelweis University, H-1089 Budapest, Hungary.
Int J Mol Sci. 2021 Jun 8;22(12):6209. doi: 10.3390/ijms22126209.
Neurodegenerative-neuroinflammatory disorders of the retina seriously hamper human vision. In searching for key factors that contribute to the development of these pathologies, we considered potential interactions among purinergic neuromodulation, glycinergic neurotransmission, and microglia activity in the retina. Energy deprivation at cellular levels is mainly due to impaired blood circulation leading to increased release of ATP and adenosine as well as glutamate and glycine. Interactions between these modulators and neurotransmitters are manifold. First, P2Y purinoceptor agonists facilitate reuptake of glycine by glycine transporter 1, while its inhibitors reduce reverse-mode operation; these events may lower extracellular glycine levels. The consequential changes in extracellular glycine concentration can lead to parallel changes in the activity of NR1/NR2B type NMDA receptors of which glycine is a mandatory agonist, and thereby may reduce neurodegenerative events in the retina. Second, P2Y purinoceptor agonists and glycine transporter 1 inhibitors may indirectly inhibit microglia activity by decreasing neuronal or glial glycine release in energy-compromised retina. These inhibitions may have a role in microglia activation, which is present during development and progression of neurodegenerative disorders such as glaucomatous and diabetic retinopathies and age-related macular degeneration or loss of retinal neurons caused by thromboembolic events. We have hypothesized that glycine transporter 1 inhibitors and P2Y purinoceptor agonists may have therapeutic importance in neurodegenerative-neuroinflammatory disorders of the retina by decreasing NR1/NR2B NMDA receptor activity and production and release of a series of proinflammatory cytokines from microglial cells.
神经退行性-神经炎症性视网膜疾病严重影响人类视力。在寻找导致这些病变发展的关键因素时,我们考虑了嘌呤能神经调制、甘氨酸能神经传递和视网膜中小胶质细胞活性之间的潜在相互作用。细胞水平的能量剥夺主要是由于血液循环受损导致 ATP 和腺苷以及谷氨酸和甘氨酸的释放增加。这些调节剂和神经递质之间的相互作用是多方面的。首先,P2Y 嘌呤能受体激动剂促进甘氨酸转运体 1 对甘氨酸的再摄取,而其抑制剂则减少反向模式操作;这些事件可能降低细胞外甘氨酸水平。细胞外甘氨酸浓度的变化会导致 NR1/NR2B 型 NMDA 受体活性的平行变化,而甘氨酸是 NMDA 受体的必需激动剂,从而可能减少视网膜中的神经退行性事件。其次,P2Y 嘌呤能受体激动剂和甘氨酸转运体 1 抑制剂可能通过减少能量受损视网膜中的神经元或神经胶质甘氨酸释放,间接抑制小胶质细胞活性。这些抑制作用可能在小胶质细胞激活中发挥作用,小胶质细胞激活存在于神经退行性疾病(如青光眼和糖尿病性视网膜病变以及年龄相关性黄斑变性)的发展过程中,或由血栓栓塞事件引起的视网膜神经元丧失。我们假设甘氨酸转运体 1 抑制剂和 P2Y 嘌呤能受体激动剂通过降低 NR1/NR2B NMDA 受体活性以及从小胶质细胞产生和释放一系列促炎细胞因子,在神经退行性-神经炎症性视网膜疾病中具有治疗意义。