NMDAR Inhibition | NMDAR Inhibitor Review

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S4023	Procaine HCl	55 mg/mL	55 mg/mL	<1 mg/mL
S2857	(-)-MK 801 maleate	<1 mg/mL	67 mg/mL	7 mg/mL
S2876	(+)-MK 801 maleate	<1 mg/mL	68 mg/mL	<1 mg/mL
S4091	Ifenprodil Tartrate	9 mg/mL	95 mg/mL	62 mg/mL
S5664	Orphenadrine Hydrochloride	-1 mg/mL	61 mg/mL	-1 mg/mL
S5287	Tiletamine Hydrochloride	-1 mg/mL	30 mg/mL	-1 mg/mL
S1330	Felbamate	<1 mg/mL	48 mg/mL	3 mg/mL
S3653	Spermidine trihydrochloride	50 mg/mL	30 mg/mL	<1 mg/mL
S4719	Kynurenic acid	<1 mg/mL	10 mg/mL	<1 mg/mL
S7072	NMDA (N-Methyl-D-aspartic acid)	30 mg/mL	5 mg/mL	<1 mg/mL
S3624	Quinolinic acid	3 mg/mL	25 mg/mL	<1 mg/mL
S4702	Sarcosine	17 mg/mL	<1 mg/mL	<1 mg/mL
S9271	Pulchinenoside A	-1 mg/mL	100 mg/mL	-1 mg/mL
S5302	6-Methoxy-2-naphthoic acid	<1 mg/mL	40 mg/mL	16 mg/mL
S5129	D-Aspartic acid	<1 mg/mL	0.01 mg/mL	<1 mg/mL

Isoform-specific Inhibitors

NMDA receptor Selective

NMDAR Products

Catalog No.	Information	Product Use Citations	Product Validations
S4023	Procaine HCl Procaine 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 K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	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.
S2857	(-)-MK 801 maleate (-)-MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with K_i of 30.5 nM.	Pharmacol Biochem Behav, 2016, 146-147:21-27 J Burn Care Res, 2017, 38(5):e842-e850 Epilepsia, 2016, 57(1):79-88	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 K_d of 37.2 nM in rat brain membranes.	J Burn Care Res, 2017, 38(5):e842-e850
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.		(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.
S5664^New	Orphenadrine Hydrochloride Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
S5287^New	Tiletamine Hydrochloride Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist.
S5032^New	Mephenesin Mephenesin is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist.
S4957^New	Linalool Linalool, a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors.
S1330	Felbamate Felbamate (Felbatol) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist.
S3653	Spermidine trihydrochloride Spermidine, 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).
S4719	Kynurenic acid Kynurenic acid, 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.
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 acid Quinolinic Acid, a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
S4702	Sarcosine Sarcosine is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.
S9271^New	Pulchinenoside A Pulchinenoside A, a natural triterpenoid saponin, is a AMPARs and NMDAR modulator.
S5302^New	6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid is an modulator of NMDAR.
S5129	D-Aspartic acid D-Aspartic acid (D-Asp) 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).

Catalog No.

Information

Product Use Citations

Product Validations

S4023

Procaine HCl

Procaine 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 K_D of 1.7 μM.

Biomol Ther (Seoul), 2016, 24(5):489-94

Catalog No.	Information	Product Use Citations	Product Validations
S2857	(-)-MK 801 maleate (-)-MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with K_i of 30.5 nM.	Pharmacol Biochem Behav, 2016, 146-147:21-27 J Burn Care Res, 2017, 38(5):e842-e850 Epilepsia, 2016, 57(1):79-88	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 K_d of 37.2 nM in rat brain membranes.	J Burn Care Res, 2017, 38(5):e842-e850
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.		(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.
S5664^New	Orphenadrine Hydrochloride Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
S5287^New	Tiletamine Hydrochloride Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist.
S5032^New	Mephenesin Mephenesin is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist.
S4957^New	Linalool Linalool, a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors.
S1330	Felbamate Felbamate (Felbatol) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist.
S3653	Spermidine trihydrochloride Spermidine, 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).
S4719	Kynurenic acid Kynurenic acid, 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 acid Quinolinic Acid, a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
S4702	Sarcosine Sarcosine 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

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 acid

Quinolinic Acid, a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.

S4702

Sarcosine

Sarcosine 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
S9271^New	Pulchinenoside A Pulchinenoside A, a natural triterpenoid saponin, is a AMPARs and NMDAR modulator.
S5302^New	6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid is an modulator of NMDAR.
S5129	D-Aspartic acid D-Aspartic acid (D-Asp) 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).

Catalog No.

Information

Product Use Citations

Product Validations

S9271^New

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NMDAR

Isoform-specific Inhibitors