Targeting N -Methyl-d-Aspartate Receptors in Neurodegenerative Diseases

-methyl-d-aspartate receptors (NMDARs) are the main class of ionotropic receptors for the excitatory neurotransmitter glutamate. They play a crucial role in the permeability of Ca ions and excitatory neurotransmission in the brain. Being heteromeric receptors, they are composed of several subunits,...

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Bibliographic Details
Published in:International journal of molecular sciences 2024-03, Vol.25 (7), p.3733
Main Authors: Carles, Allison, Freyssin, Aline, Perin-Dureau, Florent, Rubinstenn, Gilles, Maurice, Tangui
Format: Article
Language:English
Subjects:
Adults
Alzheimer Disease - drug therapy
Binding sites
Disease
Genes
Glutamic Acid
Humans
Ketamine
Life Sciences
Localization
Nervous system
Neurodegenerative Diseases - drug therapy
Neurons
Neurons and Cognition
Parkinson Disease
Permeability
Pharmaceutical sciences
Pharmacology
Physiology
Post traumatic stress disorder
Receptors, N-Methyl-D-Aspartate
Synapses
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Description
Summary:-methyl-d-aspartate receptors (NMDARs) are the main class of ionotropic receptors for the excitatory neurotransmitter glutamate. They play a crucial role in the permeability of Ca ions and excitatory neurotransmission in the brain. Being heteromeric receptors, they are composed of several subunits, including two obligatory GluN1 subunits (eight splice variants) and regulatory GluN2 (GluN2A~D) or GluN3 (GluN3A~B) subunits. Widely distributed in the brain, they regulate other neurotransmission systems and are therefore involved in essential functions such as synaptic transmission, learning and memory, plasticity, and excitotoxicity. The present review will detail the structure, composition, and localization of NMDARs, their role and regulation at the glutamatergic synapse, and their impact on cognitive processes and in neurodegenerative diseases (Alzheimer's, Huntington's, and Parkinson's disease). The pharmacology of different NMDAR antagonists and their therapeutic potentialities will be presented. In particular, a focus will be given on fluoroethylnormemantine (FENM), an investigational drug with very promising development as a neuroprotective agent in Alzheimer's disease, in complement to its reported efficacy as a tomography radiotracer for NMDARs and an anxiolytic drug in post-traumatic stress disorder.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms25073733