| 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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| S2857 |
(-)-Dizocilpine (MK 801) Maleate
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(-)-Dizocilpine (MK 801, Dizocilpine, C13737) Maleate is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
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Cancers (Basel), 2024, 16(21)3606
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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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| S3653 |
Spermidine trihydrochloride
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Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
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Cell Metab, 2023, S1550-4131(23)00341-8
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Int J Mol Sci, 2021, 22(19)10255
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Int J Mol Sci, 2021, 22(19), 10255
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| S4719 |
Kynurenic acid
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Kynurenic acid (Quinurenic acid, Kynurenate), a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist; It proved to be an antagonist at NMDA, kainate and AMPA receptors.
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Cell Prolif, 2025, e70048.
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Pharmaceuticals (Basel), 2023, 16(5)692
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Gene, 2020, 737:144434
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| S1330 |
Felbamate
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Felbamate (Felbatol, ADD-03055, W-554) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist.
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Anticancer Res, 2021, 41(2):687-697
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Neuropharmacology, 2020, 182:108371
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| S5032 |
Mephenesin
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Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is a 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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| S6644 |
Radiprodil (RGH-896)
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Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain.
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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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| 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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| S4957 |
Linalool
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Linalool (Phantol), a monoterpene compound commonly found as a major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors.
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| S5287 |
Tiletamine Hydrochloride
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Tiletamine is a lipophilc and potent veterinary anaesthetic. It is also a NMDA receptor antagonist.
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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 flavour and pharmaceutical production.
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| E4881 |
Ifenprodil
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Ifenprodil (Dilvax, RC 61-91) is a potent antagonist of N-methyl-D-aspartate (NMDA) receptor that selectively inhibits receptors containing the NR2B subunit. It exhibits potential for its use in the treatment of various neurological diseases.
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| S3535 |
Deudextromethorphan (AVP-786)
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Deudextromethorphan (AVP-786) is an active N-methyl-D-aspartate (NMDA) receptor antagonist.
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| E1771 |
Cycloleucine
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Cycloleucine is a specific antagonist of NMDA receptor (N-methyl-D-aspartate receptor coupled glycine receptor), with a Ki of 600 μM. This compound also acts as a specific inhibitor of S-adenosyl-methionine-mediated methylation. It exhibits cytostatic effects.
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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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| S0446 |
TCN 201
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TCN-201 is a selective GluN1/GluN2A (NR1/NR2A) NMDA receptor antagonist with pIC50 6.8 for NR1/NR2A and <4.3 for NR1/NR2B (GluN1/GluN2B), respectively.
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| S6731 |
Eliprodil (SL-820715)
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Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with an IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with an IC50 > 100 μM.
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| E2979 |
DL-AP5 (2-APV)
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DL-AP5 (2-APV, DL-2-Amino-5-phosphonovaleric acid) is a competitive antagonist of NMDA (N-methyl-D-aspartate) receptor. It shows significantly antinociceptive activity and specifically blocks on channels in the rabbit retina.
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