DOAJ Open Access 2024

Discovery of GluN2A subtype-selective N-methyl-d-aspartate (NMDA) receptor ligands

Liyang Jiang Na Liu Fabao Zhao Boshi Huang Dongwei Kang +2 lainnya

Abstrak

The N-methyl-d-aspartate (NMDA) receptors, which belong to the ionotropic Glutamate receptors, constitute a family of ligand-gated ion channels. Within the various subtypes of NMDA receptors, the GluN1/2A subtype plays a significant role in central nervous system (CNS) disorders. The present article aims to provide a comprehensive review of ligands targeting GluN2A-containing NMDA receptors, encompassing negative allosteric modulators (NAMs), positive allosteric modulators (PAMs) and competitive antagonists. Moreover, the ligands’ structure–activity relationships (SARs) and the binding models of representative ligands are also discussed, providing valuable insights for the clinical rational design of effective drugs targeting CNS diseases.

Topik & Kata Kunci

Therapeutics. Pharmacology

Penulis (7)

Liyang Jiang

Na Liu

Fabao Zhao

Boshi Huang

Dongwei Kang

Peng Zhan

Xinyong Liu

Format Sitasi

APA MLA BibTeX

Jiang, L., Liu, N., Zhao, F., Huang, B., Kang, D., Zhan, P. et al. (2024). Discovery of GluN2A subtype-selective N-methyl-d-aspartate (NMDA) receptor ligands. https://doi.org/10.1016/j.apsb.2024.01.004

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Informasi Jurnal

Tahun Terbit: 2024
Sumber Database: DOAJ
DOI: 10.1016/j.apsb.2024.01.004
Akses: Open Access ✓