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谷氨酸N2A和N2B亚基N-甲基-D-天冬氨酸受体（NMDARs）：它们在神经疾病中的作用及治疗性拮抗剂

GluN2A and GluN2B N-Methyl-D-Aspartate Receptor (NMDARs) Subunits: Their Roles and Therapeutic Antagonists in Neurological Diseases.

作者信息

Ladagu Amany Digal, Olopade Funmilayo Eniola, Adejare Adeboye, Olopade James Olukayode

机构信息

Department of Veterinary Anatomy, University of Ibadan, Ibadan 200284, Nigeria.

Developmental Neurobiology Laboratory, Department of Anatomy, College of Medicine, University of Ibadan, Ibadan 200284, Nigeria.

出版信息

Pharmaceuticals (Basel). 2023 Oct 30;16(11):1535. doi: 10.3390/ph16111535.

DOI:10.3390/ph16111535
PMID:38004401
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10674917/
Abstract

N-methyl-D-aspartate receptors (NMDARs) are ion channels that respond to the neurotransmitter glutamate, playing a crucial role in the permeability of calcium ions and excitatory neurotransmission in the central nervous system (CNS). Composed of various subunits, NMDARs are predominantly formed by two obligatory GluN1 subunits (with eight splice variants) along with regulatory subunits GluN2 (GluN2A-2D) and GluN3 (GluN3A-B). They are widely distributed throughout the CNS and are involved in essential functions such as synaptic transmission, learning, memory, plasticity, and excitotoxicity. The presence of GluN2A and GluN2B subunits is particularly important for cognitive processes and has been strongly implicated in neurodegenerative diseases like Parkinson's disease and Alzheimer's disease. Understanding the roles of GluN2A and GluN2B NMDARs in neuropathologies provides valuable insights into the underlying causes and complexities of major nervous system disorders. This knowledge is vital for the development of selective antagonists targeting GluN2A and GluN2B subunits using pharmacological and molecular methods. Such antagonists represent a promising class of NMDA receptor inhibitors that have the potential to be developed into neuroprotective drugs with optimal therapeutic profiles.

摘要

N-甲基-D-天冬氨酸受体（NMDARs）是对神经递质谷氨酸做出反应的离子通道，在钙离子通透性和中枢神经系统（CNS）的兴奋性神经传递中起关键作用。NMDARs由多种亚基组成，主要由两个必需的GluN1亚基（有八种剪接变体）以及调节亚基GluN2（GluN2A - 2D）和GluN3（GluN3A - B）形成。它们广泛分布于整个中枢神经系统，并参与突触传递、学习、记忆、可塑性和兴奋性毒性等重要功能。GluN2A和GluN2B亚基的存在对认知过程尤为重要，并且与帕金森病和阿尔茨海默病等神经退行性疾病密切相关。了解GluN2A和GluN2B NMDARs在神经病理学中的作用为主要神经系统疾病的潜在病因和复杂性提供了有价值的见解。这些知识对于使用药理学和分子方法开发针对GluN2A和GluN2B亚基的选择性拮抗剂至关重要。此类拮抗剂是一类有前景的NMDA受体抑制剂，有可能被开发成具有最佳治疗特性的神经保护药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59d8/10674917/3dce85adb56c/pharmaceuticals-16-01535-g018.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59d8/10674917/3dce85adb56c/pharmaceuticals-16-01535-g018.jpg

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