S2876 |
(+)-Dizocilpine (MK 801) Maleate
|
(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
-
Aging -Albany NY), 2023, 15(12):5698-5712
-
Aging (Albany NY), 2023, 15(12):5698-5712
-
Front Cell Neurosci, 2022, 16:981190
|
|
S2857 |
(-)-Dizocilpine (MK 801) Maleate
|
(-)-Dizocilpine (MK 801, Dizocilpine, C13737) Maleate is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. |
-
Aging -Albany NY), 2023, 15(12):5698-5712
-
Aging (Albany NY), 2023, 15(12):5698-5712
-
Pharmaceuticals (Basel), 2023, 16(5)692
|
|
S7072 |
NMDA (N-Methyl-D-aspartic acid)
|
NMDA(N-Methyl-D-aspartic acid)is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4. |
-
CNS Neurosci Ther, 2024, 30(2):e14611
-
Open Life Sci, 2024, 19(1):20220816
-
Aging -Albany NY), 2023, 15(12):5698-5712
|
|
S4091 |
Ifenprodil Tartrate
|
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. |
-
Cancer Sci, 2022, 113(8):2716-2726
-
Cancer Res, 2021, canres.1017.2021
-
BMC Dev Biol, 2020, 20(1):23
|
|
S2043 |
Memantine HCl
|
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. |
-
Pharmaceuticals (Basel), 2023, 16(5)692
-
Front Genet, 2022, 13:942203
-
FASEB J, 2020, 10.1096/fj.202000534R
|
|
S3653 |
Spermidine trihydrochloride
|
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). |
-
Cell Metab, 2023, S1550-4131(23)00341-8
-
Int J Mol Sci, 2021, 22(19)10255
-
Int J Mol Sci, 2021, 22(19), 10255
|
|
S4023 |
Procaine HCl
|
Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
-
Biomol Ther (Seoul), 2016, 24(5):489-94
-
Biomol Ther (Seoul), 2016, 24(5):489-94
|
|
S1330 |
Felbamate
|
Felbamate (Felbatol, ADD-03055,W-554) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist. |
-
Anticancer Res, 2021, 41(2):687-697
-
Neuropharmacology, 2020, 182:108371
|
|
S4719 |
Kynurenic acid
|
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. |
-
Pharmaceuticals (Basel), 2023, 16(5)692
-
Gene, 2020, 737:144434
|
|
S5032 |
Mephenesin
|
Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S3624 |
Quinolinic acid
|
Quinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
|
|
|
S6644 |
Radiprodil (RGH-896)
|
Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. |
|
|
S0509 |
NMDAR antagonist 1
|
NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity. |
|
|
S5129 |
D-Aspartic acid
|
D-Aspartic acid (D-Asp, Aminosuccinic acid, asparagic acid, asparaginic acid) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA). |
|
|
E1246 |
D-AP5
|
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. |
|
|
S4957 |
Linalool
|
Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors. |
|
|
S9271 |
Pulchinenoside A
|
Pulchinenoside A (Anemoside A3), a natural triterpenoid saponin, is a AMPARs and NMDAR modulator. |
|
|
S4745New |
L-Phenylalanine
|
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. |
|
|
E4881New |
Ifenprodil
|
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. |
|
|
S6907 |
Rapastinel (GLYX-13)
|
Rapastinel (GLYX-13, BV-102, TPPT-amide) is a partial agonist of N-methyl-D-aspartate receptor (NMDAR) that targeting a glycine site. Rapastinel has long-lasting antidepressant effects. |
|
|
S6224 |
(R)-Serine
|
(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. |
|
|
E1771New |
Cycloleucine
|
Cycloleucine is a specific antagonist of NMDA receptor(N-methyl-D-aspartate receptor coupled glycine receptor), with a Ki of 600 μM. Cycloleucine also acts as a specific inhibitor of S-adenosyl-methionine-mediated methylation. Cycloleucine exhibits cytostatic effects. |
|
|
S3203 |
D-Alanine
|
D-alanine (Ala, (R)-Alanine, Ba 2776, D-α-Alanine, NSC 158286) is an endogenous co-agonist at the glycine site of the N-methyl-d-aspartate (NMDA) receptor. |
|
|
S4702 |
Sarcosine
|
Sarcosine (N-methylglycine, Sarcosinic acid, Methylaminoacetic acid, Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist. |
|
|
S5664 |
Orphenadrine Hydrochloride
|
Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
|
|
S0446 |
TCN 201
|
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. |
|
|
S6731 |
Eliprodil (SL-820715)
|
Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 μM. |
|
|
S5302 |
6-Methoxy-2-naphthoic acid
|
6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR. |
|
|
E2979 |
DL-AP5 (2-APV)
|
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. |
|
|
S7072 |
NMDA (N-Methyl-D-aspartic acid)
|
NMDA(N-Methyl-D-aspartic acid)is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4. |
-
CNS Neurosci Ther, 2024, 30(2):e14611
-
Open Life Sci, 2024, 19(1):20220816
-
Aging -Albany NY), 2023, 15(12):5698-5712
|
|
S3624 |
Quinolinic acid
|
Quinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
|
|
|
S6907 |
Rapastinel (GLYX-13)
|
Rapastinel (GLYX-13, BV-102, TPPT-amide) is a partial agonist of N-methyl-D-aspartate receptor (NMDAR) that targeting a glycine site. Rapastinel has long-lasting antidepressant effects. |
|
|
S6224 |
(R)-Serine
|
(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. |
|
|
S3203 |
D-Alanine
|
D-alanine (Ala, (R)-Alanine, Ba 2776, D-α-Alanine, NSC 158286) is an endogenous co-agonist at the glycine site of the N-methyl-d-aspartate (NMDA) receptor. |
|
|
S4702 |
Sarcosine
|
Sarcosine (N-methylglycine, Sarcosinic acid, Methylaminoacetic acid, Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist. |
|
|
S2876 |
(+)-Dizocilpine (MK 801) Maleate
|
(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
- Aging -Albany NY), 2023, 15(12):5698-5712
- Aging (Albany NY), 2023, 15(12):5698-5712
- Front Cell Neurosci, 2022, 16:981190
|
|
S2857 |
(-)-Dizocilpine (MK 801) Maleate
|
(-)-Dizocilpine (MK 801, Dizocilpine, C13737) Maleate is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. |
- Aging -Albany NY), 2023, 15(12):5698-5712
- Aging (Albany NY), 2023, 15(12):5698-5712
- Pharmaceuticals (Basel), 2023, 16(5)692
|
|
S4091 |
Ifenprodil Tartrate
|
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. |
- Cancer Sci, 2022, 113(8):2716-2726
- Cancer Res, 2021, canres.1017.2021
- BMC Dev Biol, 2020, 20(1):23
|
|
S2043 |
Memantine HCl
|
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. |
- Pharmaceuticals (Basel), 2023, 16(5)692
- Front Genet, 2022, 13:942203
- FASEB J, 2020, 10.1096/fj.202000534R
|
|
S3653 |
Spermidine trihydrochloride
|
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). |
- Cell Metab, 2023, S1550-4131(23)00341-8
- Int J Mol Sci, 2021, 22(19)10255
- Int J Mol Sci, 2021, 22(19), 10255
|
|
S1330 |
Felbamate
|
Felbamate (Felbatol, ADD-03055,W-554) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist. |
- Anticancer Res, 2021, 41(2):687-697
- Neuropharmacology, 2020, 182:108371
|
|
S4719 |
Kynurenic acid
|
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. |
- Pharmaceuticals (Basel), 2023, 16(5)692
- Gene, 2020, 737:144434
|
|
S5032 |
Mephenesin
|
Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
- Cell Rep Methods, 2023, 3(10):100599
|
|
S6644 |
Radiprodil (RGH-896)
|
Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. |
|
|
S0509 |
NMDAR antagonist 1
|
NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity. |
|
|
E1246 |
D-AP5
|
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. |
|
|
S4957 |
Linalool
|
Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors. |
|
|
S4745New |
L-Phenylalanine
|
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. |
|
|
E4881New |
Ifenprodil
|
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. |
|
|
E1771New |
Cycloleucine
|
Cycloleucine is a specific antagonist of NMDA receptor(N-methyl-D-aspartate receptor coupled glycine receptor), with a Ki of 600 μM. Cycloleucine also acts as a specific inhibitor of S-adenosyl-methionine-mediated methylation. Cycloleucine exhibits cytostatic effects. |
|
|
S5664 |
Orphenadrine Hydrochloride
|
Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
|
|
S0446 |
TCN 201
|
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. |
|
|
S6731 |
Eliprodil (SL-820715)
|
Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 μM. |
|
|
E2979 |
DL-AP5 (2-APV)
|
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. |
|
|