nmda antagonist

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.

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].

NMDA Receptor Antagonist 6 (Compound 13b) functions as an antagonist at the glycine-binding site of the NMDA receptor and demonstrates cytoneuroprotective efficacy. It safeguards PC12 cells from NMDA-induced damage and apoptosis [1].

PMPA (NMDA antagonist) is a Competitive NMDA receptor antagonist.

Compound (S)-10a, a GluN2B subunit-selective NMDA receptor antagonist, exhibits a K i of 93 nM and an IC 50 of 72 nM. It is potentially useful for research into neurodegenerative diseases [1].

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic agent with brain permeability, is significant for studying neurological disorders [1].

Compound (R)-10a, an NMDA receptor antagonist, exhibits selectivity for the GluN2B subunit, possessing a Ki of 265 nM and an IC50 of 62 nM. This compound is utilized in research pertaining to neurodegenerative diseases [1].

NMDA receptor antagonist-3 is a NMDA receptor antagonist with a significan recovery rate (40.0%, at 100 μM) and safe toxicological characteristics in SH-SY5Y and human adipose mesenchymal stem cells.

NS-102 is a glutamate receptor and NMDA receptor antagonist that inhibits erythrocyanine (GluK2), which reduces glur6 receptor-mediated currents, and inhibits specific binding to the glur6 receptor.

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.

Gacyclidine (OTO311) is a small molecule N-methyl-D-aspartate (NMDA) receptor antagonist. Local injection of Gacyclidine in the cochlea inhibits salicylate-induced tinnitus and can be used to treat brain injury, spinal cord injury and tinnitus.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

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.

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.

Delucemine Hydrochloride (Delucemine) is a polyamine NMDA receptor antagonist used in the study of neurological disorders such as depression and Alzheimer's disease.

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.

Cycloleucine is an antagonist of NMDA receptor associated glycine receptor with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of S-adenosyl-methionine mediated methylation with anxiolytic and cytostatic effects.

Ifenprodil is a selective NMDA receptor (glutamate) 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.

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

Arcaine sulfate is a NMDA antagonist.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

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.

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

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).

Indantadol HCl (CHF-3381) is a NMDA antagonist and nonselective MAO inhibitor.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

AV-101 (4-Cl-KYN) , a prodrug antagonist at the glycine site of the NMDA receptor, has antidepressant activity and reduces levodopa-induced dyskinesia in MPTP monkeys.

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

MK-801 (Dizocilpine (MK-801)) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

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.

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

Alaproclate is a non-competitive NMDA receptor antagonist and a new selective 5-HT uptake inhibitor for the study of depression and dementia.

Metapramine (19560 RP) is a novel psychostimulant, an N-methyl-D-aspartate receptor (NMDA) antagonist with antidepressant and anti-injury perception activity that promotes increased levels of acetylcholine in the striatum.

SDZ 220-581 Ammonium salt is a potent, orally active, and competitive NMDA receptor antagonist (pKi: 7.7).

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).

MDL-29951 is a novel glycine antagonist for NMDA receptor activation.

QNZ46 is a non-competitive antagonist of NMDA receptors, selectively targeting NR2C NR2D subunits.

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

cis-PDA (cis PDA) is a general ionotropic receptor antagonist. cis-PDA acts by blocking NMDA, AMPA, and kainate-mediated responses.

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

Eliprodil (SL-820715)(SL-820715), a non-competitive NR2B-NMDA receptor antagonist(IC50: 1 uM), less effective for NR2A- and NR2C-containing receptors(IC50> 100 uM). It has been used in trials studying the treatment of Parkinson Disease and Movement Disorders.

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

CNQX disodium is a competitive non-NMDA receptor antagonist and competitive AMPA/kainate receptor antagonist in neuronal cultures.

NMDA-IN-1 is a potent and NR2B-selective antagonist of NMDA, with an NMDA Ki of 0.85 nM and an NR2B Ca2+ influx IC50 of 9.7 nM.

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