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NMDAR

The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells. The NMDA receptor is one of three types of ionotropic glutamate receptors. The other receptors are the AMPA and kainate receptors. It is activated when glutamate and glycine (or D-serine) bind to it, and when activated it allows positively charged ions to flow through the cell membrane. The NMDA receptor is very important for controlling synaptic plasticity and memory function.The NMDAR is a specific type of ionotropic glutamate receptor. The NMDA receptor is so named because the agonist molecule N-methyl-D-aspartate (NMDA) binds selectively to it, and not to other glutamate receptors. Activation of NMDA receptors results in the opening of an ion channel that is nonselective to cations, with a combined reversal potential near 0 mV. While the opening and closing of the ion channel is primarily gated by ligand binding, the current flow through the ion channel is voltage dependent. Extracellular magnesium (Mg2+) and zinc (Zn2+) ions can bind to specific sites on the receptor, blocking the passage of other cations through the open ion channel. Depolarization of the cell dislodges and repels the Mg2+ and Zn2+ ions from the pore, thus allowing a voltage-dependent flow of sodium (Na+) and small amounts of calcium (Ca2+) ions into the cell and potassium (K+) out of the cell.

  • Halothane
    T0954151-67-7
    Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.
    • $45
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  • Kynurenic acid
    T65135492-27-3
    Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35/CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.
    • $31
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  • CGP 78608 hydrochloride
    T107811135278-54-4In house
    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).
    • $87
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  • Glypromate acetate(32302-76-4 free base)
    T7778L
    Glypromate acetate is a neuroprotective agent, is a weak NMDA receptor agonist.
    • $59
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  • DNQX disodium salt
    T84591312992-24-7
    DNQX disodium salt is a water-soluble form of selective antagonist of non-NMDA receptor
    • $133
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  • 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
    TN5263569-83-5
    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.
    • $36
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  • LY339434 HCl
    T27947L In house
    LY339434 HCl is a low affinity GluR5 erythrocyte receptor agonist.LY339434 HCl causes rapid neuronal death primarily by affecting N-methyl-D-aspartate (NMDA) receptors.
    • $195
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  • Indantadol HCl
    T27606202914-18-9
    Indantadol HCl (CHF-3381) is a NMDA antagonist and nonselective MAO inhibitor.
    • $195
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  • N20C hydrochloride
    T230481177583-87-7
    N20C hydrochloride (2-((3,3-diphenylpropyl)amino)acetamide hydrochloride) is a non-competitive NMDA receptor open-channel blocker.
    • $84
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  • L-Cysteine S-sulfate
    T602371637-71-4
    L-Cysteine S-sulfate (S-Sulfo-L-cysteine) is an effective N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate is the substrate for cystine lyase [1].
    • $50
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  • UBP551
    T835189-35-0
    UBP551 is a potent and selective NMDA receptors modulator.
    • $50
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  • Orphenadrine
    T6859983-98-7In house
    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.
    • $52
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  • Dalzanemdor
    T628391629853-48-0In house
    Dalzanemdor (SAGE-718) is an NMDA receptor-positive modulator of metabolism that can be used to study Huntington's chorea, Alzheimer's disease, and cognitive dysfunction.
    • $670
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  • Neboglamine hydrochloride
    T606122759182-59-5In house
    Neboglamine hydrochloride (CR-2249 hydrochloride) is an orally active positive modulator of NMDA receptors with neuroprotective activity, enhances cognition, and may be used in studies of schizophrenia and lupus erythematosus.
    • $227
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  • Alaproclate
    T6901360719-82-6In house
    Alaproclate is a non-competitive NMDA receptor antagonist and a new selective 5-HT uptake inhibitor for the study of depression and dementia.
    • $293
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  • Rapastinel acetate
    T3407L491872-39-0
    Rapastinel acetate is a modulator of N-methyl-D-aspartate (NMDA) receptor and a partial agonist of glycine site long-lasting antidepressant effects.
    • $195
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  • Delucemine Hydrochloride
    T27143186495-99-8In house
    Delucemine Hydrochloride (Delucemine) is a polyamine NMDA receptor antagonist used in the study of neurological disorders such as depression and Alzheimer's disease.
    • $293
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  • Dizocilpine
    T625977086-21-6
    MK-801 (Dizocilpine (MK-801)) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
    • $57
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  • UK-240455
    T13248178908-09-3In house
    UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improved motor function in Parkinson's disease models, and is a potential candidate compound for treatment of Parkinson's disease.
    • $350
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  • 3-MATIDA
    T3486518357-51-2In house
    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.
    • $37
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  • AV-101
    T26686153152-32-0In house
    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.
    • $192
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  • UBP710
    T249181333111-40-2
    UBP710 is an effective and selective NMDA receptor modulator.
    • $148
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  • BDBM50597431
    T28367L11629853-49-1In house
    BDBM50597431 is an NMDA receptor modulator that may have can be used to study Alzheimer's disease and Parkinson's syndrome.
    • $195
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  • PEAQX tetrasodium hydrate
    T16451
    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.
    • $71
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  • Bupivacaine hydrochloride monohydrate
    T8064173360-54-0
    Bupivacaine hydrochloride monohydrate is a potent NMDA receptor inhibitor of sodium, L-calcium, and potassium channels.Bupivacaine hydrochloride monohydrate inhibits SCN5A channels and is commonly used in the study of chronic pain.
    • $195
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  • Ro 25-6981
    T12758169274-78-6
    Ro 25-6981 is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit with IC50s of 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Ro 25-6981 can be used in studies about Parkinson's disease.
    • $48
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  • Gacyclidine
    T2739768134-81-6In house
    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.
    • $85
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  • Ifenprodil
    T1186L23210-56-2
    Ifenprodil (RC61-91) is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, Ifenprodil inhibits GIRK channels and interacts with alpha1 adrenergic, serotonin, and sigma receptors.
    • $186
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  • NP10679
    T734472914889-88-4In house
    NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.
    • $293 TargetMol
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  • CNS-5161 hydrochloride
    T10852160756-38-7In house
    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.
    • $848
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  • SDZ 220-040
    T23344174575-40-7In house
    SDZ 220-040 is a selective mammalian NMDA receptor antagonist that induces a partially gravity-free mode of root growth.
    • $62
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  • Aptiganel
    T26645137159-92-3In house
    Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.
    • $293
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  • S1R agonist 2
    T72059150085-21-5In house
    S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.
    • $39
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  • Nelonemdaz
    T16286640290-67-1In house
    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.
    • $64 TargetMol
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  • SDZ 220-040 ammonium
    T23344L In house
    SDZ 220-040 ammonium is a competitive glutamate ionotropic receptor NMDA antagonist used in the study of neurological disorders.
    • $259
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  • 7-Chlorokynurenic acid
    T10191L18000-24-3In house
    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.
    • $38
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  • ZL006
    T172931181226-02-7
    ZL006 is an effective inhibitor of nNOS/PSD-95 interaction. ZL006 also inhibits NMDA receptor-mediated NO synthesis.
    • $32
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  • Urethane
    T005151-79-6
    Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.
    • $31
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  • QNZ46
    T23621237744-13-6
    QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist.
    • $47
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  • Transtorine
    T862613593-94-7
    Transtorine (1,4-DIHYDRO-4-OXOQUINOLINE-2-CARBOXYLIC ACID) is a GluR and NMDA inhibitor.
    • $39
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  • L-689560
    T15684139051-78-8
    L-689560 is widely used as a radiolabeled ligand in binding studies and used to study the roles of NMDA receptors in normal neurological processes as well as in diseases. At the GluN1 glycine binding site, L-689560 is an effective N-methyl-D-aspartate (NM
    • $668
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  • Traxoprodil
    TQ0233134234-12-1
    Traxoprodil (CP101606) is a selective NMDA antagonist and protects hippocampal neurons (IC50: 10 nM).
    • $47
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  • 5,7-Dichlorokynurenic acid
    T22517131123-76-7
    5,7-Dichlorokynurenic acid (5,7-dichlorokynurenic acid sodium) is an NMDA receptor antagonist.
    • $39
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  • BZAD01
    T25196305339-41-7
    BZAD01 is a selective NMDA NR1A/2B receptor antagonist.
    • $115
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  • Rapastinel Trifluoroacetate
    T58191435786-04-1
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties.
    • $55
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  • 6-Methoxy-2-naphthoic acid
    T05562471-70-7
    6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR.
    • $29
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  • Mephenesin
    T001559-47-2
    Mephenesin (Cresoxydiol) is a centrally acting muscle relaxant with a short duration of action.
    • $42
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  • NT 13 acetate
    TP1023L
    NT 13 acetate is a partial agonist of NMDA receptor and can be used for research on depression, anxiety, and other related diseases.
    • $497
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  • MRZ 2-514
    T12110202808-11-5
    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.
    • $347
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  • CIQ
    T14971486427-17-2
    CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. EC50 value: 2.7 μM for NR2C and 2.8 μM for NR2D.
    • $34
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