Receptor to Glutamate NMDA-Type: The Functional Diversity of the NR1 Isoforms and Pharmacological Properties

Mario      Eduardo Flores-Soto; Verónica      Chaparro-Huerta; Martha      Escoto-Delgadillo; Mónica      Elisa Ureña-Guerrero; Antoni      Camins; Carlos      Beas-Zarate

doi:10.2174/1381612811319380003

Abstract

Glutamic acid (Glu) is the major excitatory neurotransmitter in the central nervous system, and interacts with two classes of receptor: metabotropic and ionotropic receptors. Ionotropic receptors are divided according to the affinity of their specific agonists: Nmethyl- D-aspartate (NMDA), amino acid-3-hydroxy-5-methyl-4-isoxazole acid (AMPA) and kainic acid (KA). NMDA receptors (NMDA-R) are macromolecular structures that are formed by different combinations of subunits: NMDAR1 (NR1), NMDAR2 (NR2) and NMDAR3 (NR3). The study of this receptor has aroused great interest, partly due to its role in synaptic plasticity but mainly because of its permeability to the Ca2+ ion. This review examines the molecular composition of NMDA-R and the variants of NR1 subunit editing in association with NR2 subunit dimers, which form the main components of this receptor. Their composition, structure, function and distinct temporal and spatial expression patterns demonstrate the versatility and diversity of functionally different isoforms of NR1 subunits and the various pharmacological properties of the NR2 subunit. Finally, the involvement of NMDA-R in the excitotoxicity phenomenon, as well as, its expression changes under these conditions as neuronal response are also discussed.

Keywords: NMDA receptor, NR1 Subunit, NR2 Subunit, Isoform, Excitotoxicity

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