nmdar

NMDAR antagonist 1 is an orally active, NR2B-selective NMDAR antagonist.

NMDAR/TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR/TRPM4 interaction.NMDAR/TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.NMDAR/TRPM4-IN-2 has neuroprotective activity against NMDA-induced hippocampal neuronal cell death and mitochondrial dysfunction. NMDAR/TRPM4-IN-2 showed neuroprotective activity against NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons with an IC50 value of 2.1 μM.

NMDAR HDAC-IN-1 (Compound 9d) is a potent dual inhibitor of N-methyl-D-aspartate receptors (NMDARs) and histone deacetylases (HDACs), with a high affinity for NMDARs (Ki = 0.59 μM) and significant inhibitory effects on various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 2.67 μM, 8.00 μM, 2.21 μM, 0.18 μM, and 0.62 μM, respectively; additionally, it efficiently crosses the blood-brain barrier [1].

GluN2B-NMDAR Antagonist-1, an orally active compound, functions as a GluN2B-NMDAR antagonist with neuroprotective properties. It is applicable in the research of ischemic injury [1].

(Rac)-NMDAR antagonist 1 is a racemate of NMDAR antagonist 1, a potent, orally active, NR2B-selective NMDAR antagonist.

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

Nandrolone decanoate (19-Nortestosterone decanoate) is the decanoate salt form of nandrolone, an anabolic steroid analog of testosterone with androgenic, anabolic, and erythropoietin-stimulating effects. Nandrolone binds to and activates specific nuclear androgen receptors in responsive tissues, including the prostate, seminal vesicles, scrotum, penis, larynx, hair follicles, muscle, and bone.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

D-Serine ((R)-Serine), an endogenous amino acid, is a potent co-agonist at the NMDA glutamate receptor.

Sarcosine (Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1/GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

Tat-NR2B9c acetate (NA-1 acetate) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c acetate disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c acetate also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A 2A was 270 nM and 29600 nM against hNMDAR 1A 2B, respectively.

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

PEAQX (NVP-AAM077)(NVP-AAM 077) is an effective and orally available NMDA antagonist. It can inhibit human NMDA receptors for 1A/2A(IC50: 270 nM), rather than 1A/2B(29, 600 nM).

Felbamate (W-554) is an Anti-epileptic Agent. The physiologic effect of felbamate is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Traxoprodil (CP101606) is a selective NMDA antagonist and protects hippocampal neurons (IC50: 10 nM).

TCN 201 is a selective antagonist of NMDA receptors containing the NR2A subunit.

6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR.

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

IC87201 is a nNOS-PDZ/PSD-95-PDZ inhibitor. IC87201 showed great promise in cellular experiments and animal models of ischemic stroke and pain.

GNE-9278 is a highly selective NMDAR orthosteric modulator that targets the GluN1 transmembrane structural domain (TMD), enhancing peak current and agonist affinity in activated NMDAR.

TP-050 is a potent, selective NMDAR agonist that is orally active, showing EC50 values of 0.51 µM for GluN2A and 9.6 µM for GluN2D. This compound can cross the blood-brain barrier (BBB), enhancing hippocampal long-term (LTP) potentiation and neuronal signal transmission.

NMDA receptor antagonist 4 (IIc) is an uncompetitive, voltage-dependent, orally active NMDAR blocker with an IC50 of 1.93 μM. It shows positive predicted blood-brain-barrier (BBB) permeability and can be used in Alzheimer's disease research[1].

GNE 5729 is an NMDAR of brain permeable positive allosteric modulator (EC50: 37 nM for GluN2A; 4.7 and 9.5 μM for GluN2C and GluN2D, respectively).

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

NYX-2925, an orally active NMDAR (N-methyl-D-aspartate receptor) modulator, enhances activated Src levels and Src phosphorylation at GluN2A and GluN2B sites in the mPFC (medial prefrontal cortex), without affecting CAMKII (Ca2+/calmodulin-dependent protein kinase II) or exhibiting addictive or sedative/ataxic side effects. It is utilized in the study of various CNS (central nervous system) disorders mediated by NMDA receptors.

Withaphysalin D, isolated from water lilies, is a selective antagonist for the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B with neuroprotective properties. This compound is capable of crossing the blood-brain barrier [1].

GluN1 (359-378), an antibody targeting the N-methyl-D-aspartate receptor (NMDAR), can cross the blood-brain barrier and is used in research on immune-based therapies for anti-NMDAR encephalitis [1].

6-Hydroxykynurenic acid (6-HKA), a kynurenic acid (KYNA) derivative isolated from Ginkgo leaves, functions as a low-affinity NMDAR antagonist with an IC50 of 59 μM [1].

GNE 0723 is an NMDAR brain permeable positive allosteric modulator (EC50: 21 nM for GluN2A; 7.4 and 6.2 μM for GluN2C and GluN2D, respectively).

Gavestinel (GV 150526) is a non-competitive NMDA receptor antagonist that is potent, selective and orally active.Gavestinel binds to the glycine site of the NMDA receptor with a binding affinity (pKi value) of 8.5.Gavestinel is used in acute ischaemic stroke studies.

Neurogranin (48-76), mouse, is a peptide comprising residues 48-76 of Neurogranin, a post-synaptically exclusive calmodulin-binding protein that mediates NMDAR-driven synaptic plasticity by regulating the calcium-calmodulin (Ca2+-CaM) pathway [1].

Tat-NR2BAA TFA serves as the inactive control peptide for Tat-NR2B9c, featuring a comparable sequence with a crucial distinction: a double-point mutation in its COOH-terminal tSXV motif. This alteration renders Tat-NR2BAA TFA unable to bind to PSD-95, in contrast to Tat-NR2B9c. The latter is a membrane-permeant peptide that impedes PSD-95/NMDAR interaction, specifically detaching NR2B- and/or NR2A-type NMDARs from PSD-95 [1].

TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, protecting neurons against oxidative stress and NMDAR-mediated excitotoxicity, making it valuable for neuroprotection research studies [1].

Rapastinel (TPPT-amide) (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator.

Tacrine is a indirect cholinergic agonist and centrally acting anticholinesterase. Tacrine hydrochloride hydrate is an inhibitor of acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.

DQP-26, a potent negative allosteric modulator of NMDA receptors (NMDARs), exhibits IC50 values of 0.77 μM for GluN2C and 0.44 μM for GluN2D subunits, indicating potential application in research on NMDAR-associated neurological diseases [1].

UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent

Remacemide hydrochloride is a NMDA receptor antagonist.

Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.

VSGLNPSLWSIFGLQFILLWLVSGSRHYLW, a 30-amino-acid peptide, mirrors the C-terminal domain of α2δ-1 and is recognized as the α2δ-1Tat peptide. It disrupts the α2δ-1 - NMDAR interaction both in vitro and in vivo, offering a potential research tool for neuropathic pain studies [1].

VSGLNPSLWSIFGLQFILLWLVSGSRHYLW (TFA), a 30-amino-acid peptide, mimics the C-terminal domain of α2δ-1, known as α2δ-1Tat peptide. This compound disrupts the α2δ-1 - NMDAR interaction both in vitro and in vivo, demonstrating potential utility in neuropathic pain research [1].

NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.

GluN1 (356-385) is an antigenic peptide implicated in N-methyl-D-aspartate receptor (NMDAR) encephalitis, shown to decrease NMDAR surface cluster density in hippocampal neurons, and serves as a tool to investigate the pathogenesis of anti-NMDAR encephalitis [1].

Rislenemdaz (CERC-301) (CERC-301) is an antagonist of the N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B).