nmda receptor antagonist 2

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound is valuable in scientific investigations of neuropathic pain and Parkinson's disease.

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.

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.

Co 101244 hydrochloride (4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride) is an NR2B-containing NMDA receptor antagonist.

EP2 receptor antagonist-2 (CID891729) is a compound that blocks EP2 receptor activation by PGE2 and reduces lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).

DNQX disodium salt is a water-soluble form of selective antagonist of non-NMDA receptor

MRZ 2-514 (8-bromo-4,5-dihydroxypyridazino[4,5-b]quinolin-1-one) is a strychnine-insensitive modulatory site of the NMDA receptor (glycineB)antagonist with Ki of 33 μM.

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

DL-AP5 (2-APV) lithium is a competitive antagonist of the NMDA (N-Methyl-D-aspartate) receptor. It exhibits notable analgesic activity and specifically blocks channels in the rabbit retina.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine with potential to treat Alzheimer's disease, prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors, and is a potent GABA A receptor antagonist[1] [2] [3].

Ensaculin is a NMDA antagonist and a 5HT1A agonist potentially for the treatment of Alzheimer's disease (AD). Ensaculin showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It e

Aminoadipic acid (DL-2-Aminoadipic acid) (2-aminoadipate) is a metabolite in the principal biochemical pathway of lysine. It is an intermediate in the metabolism (i.e. breakdown or degradation) of lysine and saccharopine. It antagonizes neuroexcitatory activity modulated by the glutamate receptor N-methyl-D-aspartate (NMDA). Aminoadipic acid has also been shown to inhibit the production of kynurenic acid, a broad spectrum excitatory amino acid receptor antagonist, in brain tissue slices.

Procyclidine (Tricyclamol; (±)-Procyclidine) is an anticholinergic agent that functions as a muscarinic receptor antagonist and an N-methyl-D-aspartate (NMDA) antagonist. It is used in studies of Parkinson's disease and related psychiatric disorders, including Soman-induced epilepsy [1][2].

GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg kg. GYKI 52466 (30 mg kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

Flupirtine-d4 (D 9998-d4) hydrochloride, the deuterium-labeled version of Flupirtine (D 9998) hydrochloride, is a selective neuronal potassium channel opener with NMDA receptor antagonist properties [1] [2].

AChE Aβ-IN-2 (compound 33) is a potent, orally active acetylcholinesterase (AChE) inhibitor (IC50: 135 nM), an NMDA receptor antagonist (GluN1-1b GluN2B subunit combination, IC50: 5.054 μM), inhibits Aβ aggregation, demonstrates favorable blood-brain barrier permeability, and enhances cognitive and spatial memory in a rat model [1].