NMDAR
Inhibitory Selectivity
Isoform-specific Inhibitors
NMDAR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S4023 |
Procaine HClProcaine (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. |
Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
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| S2857 |
(-)-MK 801 maleate(-)-MK-801 (Dizocilpine, C13737) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. |
The NMDA receptor is involved in the neuroprotective effect of Res. MK 801 (2 mg/kg) was injected respectively at 30 min prior to cerebral ischemia or at 30 min prior to the administration of Res at 1 or 24 h pre-MCAO. (A) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 1 h pre-MCAO. (B) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 24 h pre-MCAO. n = 5 rats at each group.
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| S2876 |
(+)-MK 801 maleate(+)-MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
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| S4091 |
Ifenprodil TartrateIfenprodil 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. |
(B) Vehicle-treated rats, BDNF-treated rats, rats pre-treated with CTX-B and rats pre-treated with Ifenprodil showed equivalenttime in the pairing chambers prior to the conditioning day. There were no differences in these groups;thus,the preconditioning values were pooled for graphical representation. Only BDNF-treated rats showed a clear preference for the chamber paired with spinal clonidine (10 g). *P < 0.05, compared with pre-conditioning, two-way ANOVA, F(1,1,1/20) = (23.25, 16.89, 10.97), n = 6/group. (C) Difference score, indicates that application of BDNF in intact rats increased the time spent in the clonidine-paired chamber, while pre-injection of CTX-B or Ifenprodil into the rACC attenuated the difference score. #P < 0.05, one-way ANOVA, F(3,20) = 15.38, n = 6/group. Data are expressed as the mean ± SEM.
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| S6644 |
Radiprodil (RGH-896)Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. |
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| S2043 |
Memantine HClMemantine 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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| S1330 |
FelbamateFelbamate (Felbatol, ADD-03055) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist. |
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| S4957 |
LinaloolLinalool (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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| S5287 |
Tiletamine HydrochlorideTiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist. |
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| S3653 |
Spermidine trihydrochlorideSpermidine (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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| S5032 |
MephenesinMephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
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| S5664 |
Orphenadrine HydrochlorideOrphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
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| S0446 |
TCN 201TCN-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)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. |
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| S4719 |
Kynurenic acidKynurenic 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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| 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. |
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| S3624 |
Quinolinic acidQuinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor. |
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| S6907New |
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. |
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| S6224 |
(R)-Serine(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. (R)-Serine acts as obligatory coagonist at the glycine site associated with the N-methyl-D-aspartate subtype of glutamate receptors (NMDAR) and has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration. |
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| S3203 |
D-AlanineD-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. |
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| S4702 |
SarcosineSarcosine (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. |
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| S5129 |
D-Aspartic acidD-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). |
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| S9271 |
Pulchinenoside APulchinenoside A (Anemoside A3), a natural triterpenoid saponin, is a AMPARs and NMDAR modulator. |
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| S5302 |
6-Methoxy-2-naphthoic acid6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S4023 |
Procaine HClProcaine (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. |
Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2857 |
(-)-MK 801 maleate(-)-MK-801 (Dizocilpine, C13737) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. |
The NMDA receptor is involved in the neuroprotective effect of Res. MK 801 (2 mg/kg) was injected respectively at 30 min prior to cerebral ischemia or at 30 min prior to the administration of Res at 1 or 24 h pre-MCAO. (A) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 1 h pre-MCAO. (B) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 24 h pre-MCAO. n = 5 rats at each group.
|
|
| S2876 |
(+)-MK 801 maleate(+)-MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
||
| S4091 |
Ifenprodil TartrateIfenprodil 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. |
(B) Vehicle-treated rats, BDNF-treated rats, rats pre-treated with CTX-B and rats pre-treated with Ifenprodil showed equivalenttime in the pairing chambers prior to the conditioning day. There were no differences in these groups;thus,the preconditioning values were pooled for graphical representation. Only BDNF-treated rats showed a clear preference for the chamber paired with spinal clonidine (10 g). *P < 0.05, compared with pre-conditioning, two-way ANOVA, F(1,1,1/20) = (23.25, 16.89, 10.97), n = 6/group. (C) Difference score, indicates that application of BDNF in intact rats increased the time spent in the clonidine-paired chamber, while pre-injection of CTX-B or Ifenprodil into the rACC attenuated the difference score. #P < 0.05, one-way ANOVA, F(3,20) = 15.38, n = 6/group. Data are expressed as the mean ± SEM.
|
|
| S6644 |
Radiprodil (RGH-896)Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. |
||
| S2043 |
Memantine HClMemantine 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. |
||
| S1330 |
FelbamateFelbamate (Felbatol, ADD-03055) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist. |
||
| S4957 |
LinaloolLinalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors. |
||
| S5287 |
Tiletamine HydrochlorideTiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist. |
||
| S3653 |
Spermidine trihydrochlorideSpermidine (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). |
||
| S5032 |
MephenesinMephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
||
| S5664 |
Orphenadrine HydrochlorideOrphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
||
| S0446 |
TCN 201TCN-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. |
||
| S4719 |
Kynurenic acidKynurenic 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
||
| S3624 |
Quinolinic acidQuinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor. |
||
| S6907New |
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. (R)-Serine acts as obligatory coagonist at the glycine site associated with the N-methyl-D-aspartate subtype of glutamate receptors (NMDAR) and has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration. |
||
| S3203 |
D-AlanineD-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 |
SarcosineSarcosine (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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5129 |
D-Aspartic acidD-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). |
||
| S9271 |
Pulchinenoside APulchinenoside A (Anemoside A3), a natural triterpenoid saponin, is a AMPARs and NMDAR modulator. |
||
| S5302 |
6-Methoxy-2-naphthoic acid6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR. |
