| E8008 |
QNZ46
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QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D NR2A)Target: NR2D, NR2C, NR2Ain vitro: QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit.
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| E7521 |
MDL-29951
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MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
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| S2876 |
(+)-Dizocilpine (MK 801) Maleate
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(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.(+)-Dizocilpine (MK 801) Maleate can be used to induce animal models of Schizophrenia.
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Theranostics, 2025, 15(14):6901-6918
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Aging -Albany NY), 2023, 15(12):5698-5712
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Aging (Albany NY), 2023, 15(12):5698-5712
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| S4091 |
Ifenprodil Tartrate
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Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
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J Immunother Cancer, 2024, 12(11)e009805
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Cancer Sci, 2022, 113(8):2716-2726
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Cancer Res, 2021, canres.1017.2021
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| S2043 |
Memantine HCl
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Memantine HCl is an antagonist of NMDAR. It is also a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with IC50 of 1.12 μM and 242.4 μM, Ki of 0.51 μM and 84.4 μM, respectively.
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Pharmaceuticals (Basel), 2023, 16(5)692
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Front Genet, 2022, 13:942203
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FASEB J, 2020, 10.1096/fj.202000534R
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| S1334 |
Flupirtine maleate
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Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
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Assay Drug Dev Technol, 2019, 17(7):310-321
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Elife, 2015, 4
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| S5032 |
Mephenesin
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Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist.
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Cell Rep Methods, 2023, 3(10):100599
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| S0509 |
NMDAR antagonist 1
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NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity.
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| E1259 |
DNQX
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DNQX is an AMPA receptor antagonist that prevents excess calcium influx via voltage-gated calcium channels.
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| E1246 |
D-AP5
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D-AP5 (D-APV; D-2-Amino-5-phosphonovaleric acid) is a selective and competitive NMDA receptor antagonist that inhibits the glutamate binding site of NMDA receptors.
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| E0484 |
CNQX
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CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. This compound is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). It shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
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| S4957 |
Linalool
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Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors.
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| S4745 |
L-Phenylalanine
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L-Phenylalanine is an essential amino acid and a competitive antagonist against NMDAR glycine- and glutamate-binding sites with a Kb of 573 μM. It is widely used in food flavor and pharmaceutical production.
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| E1050 |
PEAQX
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PEAQX (NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM).
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| S5664 |
Orphenadrine Hydrochloride
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Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
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| S9686 |
NBQX (FG9202)
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NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
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