nmdar

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.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

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.

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

Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.

Bacopaside I is a saponin isolated from Bacopa monniera. Bacopaside I is a modulator of Aquaporin-1 channel, has neuroprotective functions, it has anti-Alzheimer's disease, it ameliorates cognitive impairment in APP/PS1 mice via immune-mediated clearance of α2-amyloid,exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.

NMDAR antagonist 2 (compound 3I) is a blood-brain barrier permeable antagonist of NMDA receptors, exhibiting IC50 values of 4.42 μM and 214.75 μM at membrane potentials of -60 mV and 40 mV, respectively, for hGluN1/hGluN2A. This compound has been shown to mitigate hippocampal damage.

NMDAR antagonist 5 (Compound A17) is a multi-target antagonist that acts on NMDAR and monoamine transporters (SERT, DAT, and NET). It demonstrates strong NMDAR antagonistic efficacy (IC50= 0.3 μM) and effective activity on monoamine transporters (SERT IC50= 1.1 μM, DAT IC50= 0.7 μM, NET IC50= 2.7 μM). NMDAR antagonist 5 exhibits high safety with low toxicity (hepatic and renal toxicity IC50> 100 μM; cardiac toxicity IC50= 24.5 μM). It has antidepressant properties and is useful for depression research.

GluN2B-NMDAR antagonist-2 (compound S-58) is an effective and selective NMDAR-GluN2B antagonist that can cross the blood-brain barrier, with an IC50 value of 74.01 nM. It exhibits mild cytotoxicity and reduces both infarct size and neurological deficit scores in the brain, indicating its potential for stroke research.

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

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].

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

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].

CNS-5161 hydrochloride (CNS 5161A) is a new antagonist of NMDA ion-channel. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

D-AP5 (D-APV) is an NMDA receptor antagonist.

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).

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

GV-196771A A novel NMDA receptor glycine site antagonist with potent antinociceptive activity.

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.

Nelonemdaz (Neu2000) is an NMDA receptor antagonist with antioxidant activity and neuroprotective activity used in the study of cerebral infarction reperfusion injury and acute ischemic stroke.

RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.

SDZ 220-040 is a selective mammalian NMDA receptor antagonist that induces a partially gravity-free mode of root growth.

SDZ 220-040 ammonium is a competitive glutamate ionotropic receptor NMDA antagonist used in the study of neurological disorders.