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A peer-reviewed article of this preprint also exists.
This version is not peer-reviewed
Submitted:
10 February 2024
Posted:
12 February 2024
You are already at the latest version
ABD | agonist binding domain |
AD | Alzheimer's disease |
AMPAR | α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor |
Aβ | amyloid-β |
BDNF | brain-derived neurotrophic factor |
CaMKII | calcium moduling kinase II |
cAMP | 3’,5’-adenosine monophosphate |
cGMP | 3’,5’-guanosine monophosphate |
CNS | central nervous system |
CREB | cAMP response element binding protein |
CTD | carboxyl C-terminal domain |
DYRK1A | dual specificity tyrosine-phosphorylation-regulated kinase 1 |
EAAT | excitatory amino acid transporter |
ERK1/2 | extracellular signal-regulated protein kinase 1/2 |
FENM | fluoroethylnormemantine |
GABA | γ-aminobutyric acid |
HD | Huntington's disease |
HEK-293 | human embryonic kidney 293 cells |
L-Dopa | L-3,4-dihydroxyphenylalanine |
LTD | long-term depression |
LTP | long-term potentiation |
MAPK | mitogen-activated protein kinases |
NMDAR | N-methyl-D-aspartate receptor |
PCP | phencycline |
PD | Parkinson's disease |
PET | positron emission tomography |
PKA | protein kinase A |
PSD-95 | postsynaptic density protein 95 |
PTSD | post-traumatic-stress-disorder |
RCPG | G protein-coupled receptor |
SANT | sodium-coupled neutral amino acid transporter |
tPA | tissue-type plasminogen activator |
Compounds | Modulator | Selectivity | Action | References |
---|---|---|---|---|
D-AP5 | Hight selective competitive antagonist | GluN2A | Inhibits excitatory response. Impacts behavioural learning, blocks plasticity (LTP). | [90,91,92] |
Riluzole | Competitive antagonist | GluN1/GluN2B | Indirect block of NMDAR. Protect from motor deficit | [98,99,100] |
Phencyclidine | Selective uncompetitive antagonist | GluN2B/D(PCP site) | Induces psychotic and dissociative schizophrenia-like symptoms. Impairs NMDAR neurotransmission in vivo. | [93] |
Ketamine | Uncompetitive antagonist | GluN2B/D(PCP site) | Applied in post-synapse : inhibits excitatory pyramidal neuron in extra-synaptic GluN2B. Applied in pre-synapse: inhibits GluN2D in interneuron (induces disinhibition of glutamate release in post-synapse). Up-regulates hippocampal AMPARs (GluA1/GluA2). antidepressant. | [95,101] |
Dizocilpine | Uncompetitive antagonist | GluN2B/D(PCP site) | Anticonvulsant, antidepressant. Induces memory impairments. | [97,102] |
Ifenprodil | Uncompetitive antagonist | GluN1/GluN2B | Blocks GluN2B (140-fold preference for NR2B over NR2A subunits). Induces an inhibition of GluN2R receptor currents. anti-Parkinsonian effect. | [103,104,105] |
Memantine | Uncompetitive antagonist | GluN1/GluN2B | Blocks GluN2B extra-synaptic and induces glutamatergic excitotoxicity. Used for moderate-to-severe AD. | [106,107] |
Amantadine | Uncompetitive antagonist | GluN1/GluN2B | Blocks GluN1/GluN2B by accelerating channel closure during channel block. Used as antiparkinsonian drug | [108] |
Dextrometorphan | Uncompetitive antagonist | GluN2A | Blocks GluN2A subunit. Prevent neuronal damage and modulates pain sensation | [109,110,111,112,113] |
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