Signaling Pathway

NMDA Receptor

NMDA Receptor

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The N-methyl-D-aspartate receptor (NMDA receptor, NMDAR), a glutamate receptor, is the predominant molecular device for controlling synaptic plasticity and memory function. The NMDAR is a specific type of ionotropic glutamate receptor. NMDA is the name of a selective agonist that binds to NMDA receptors but not to other glutamate receptors. Activation of NMDA receptors results in the opening of an ion channel that is nonselective to cations with an equilibrium potential near 0 mV. A property of the NMDA receptor is its voltage-dependent activation, a result of ion channel block by extracellular Mg2+ & Zn2+ ions. This allows the flow of Na+ and small amounts of Ca2+ ions into the cell and K+ out of the cell to be voltage-dependent. The NMDA receptor is a non-specific cation channel that can allow the passage of Ca2+ and Na+ into the cell and K+ out of the cell. NMDA receptors are modulated by a number of endogenous and exogenous compounds and play a key role in a wide range of physiological (e.g., memory) and pathological processes (e.g.,excitotoxicity).

NMDA Receptor Inhibitors & Modulators (31)

Product Name Catalog No. Brief Description
(+)-MK 801 Maleate

HY-15084

Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM
IC50 Value: 30.5 nM[1].

(-)-MK 801 Maleate

HY-15084A

(-)-MK 801 Maleate is the enantiomer of (+)-MK-801; (+)-MK-801 is a highly potent and selective non-competitive NMDA glutamate receptor antagonist .

CIQ

HY-18699

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.

Dextromethorphan hydrobromide

HY-B0620

Dextromethorphan hydrobromide is an antitussive drug.

Dextromethorphan hydrobromide hydrate

HY-B1333

Dextromethorphan hydrobromide hydrate is an antitussive drug.

Eliprodil

HY-12881

Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).

Felbamate

HY-B0184

Felbamate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .

Felbamate hydrate

HY-B0184A

Felbamate hydrate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .

IC87201

HY-100457

IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

Ifenprodil tartrate

HY-12882A

Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.

L-701324

HY-18698

L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.

MDL 105519

HY-15085

MDL 105519 is a potent and selective inhibitor of [3H]glycine binding to the NMDA receptor with Kd of 3.89 nM.

MDL-29951

HY-16312

MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo.

Memantine hydrochloride

HY-B0365A

Memantine, an amantadine derivative with low to moderate-affinity for NMDA receptors, is used for the treatment of Alzheimer's disease.

Mephenesin

HY-B1283

Mephenesin is an NMDA receptor antagonist, is a centrally acting muscle relaxant.

NMDA

HY-17551

NMDA(N-Methyl-D-aspartic acid) is an amino acid derivative that acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.

NMDA-IN-1

HY-12962

NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.

Orphenadrine citrate

HY-B0369A

Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

Orphenadrine hydrochloride

HY-B1126

Orphenadrine hydrochloride is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 6.0 ±0.7 μM.

PEAQX

HY-12294

PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).