NMDAR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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 a 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 an AMPARs and NMDAR modulator.
S5287 Tiletamine Hydrochloride Tiletamine is a lipophilc and potent veterinary anaesthetic. It is also a NMDA receptor antagonist.
S4745 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 flavour and pharmaceutical production.
E4881 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 targets a glycine site, and it has long-lasting antidepressant effects.
S3535 Deudextromethorphan (AVP-786) Deudextromethorphan (AVP-786) is an active N-methyl-D-aspartate (NMDA) receptor antagonist.
S6224 (R)-Serine (R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. This compound 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.
E1771 Cycloleucine 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.
E1050 PEAQX 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).
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 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 an IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with an IC50 > 100 μM.
S5302 6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is a 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.
E3792 Lavandula Angustifolia Extract Lavandula Angustifolia Extract is drawn from Lavandula angustifolia, which has a positive impact on the tetanised NMDA receptor-mediated synaptic transmission in both normal and, especially, Alzheimeric animals.
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
Verified customer review of Procaine HCl