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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.

  • 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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  • 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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  • D-AP5
    T1093079055-68-8
    D-AP5 (D-APV) is an NMDA receptor antagonist.
    • $30
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  • Caroverine hydrochloride
    T913355750-05-5
    Caroverine hydrochloride (Caroverine HCL) is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. It is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action, and can be used for the research of inner ear tinnitus.
    • $39
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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.
    • $30
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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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  • 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.
    • $509
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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 TargetMol
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  • Dizocilpine Maleate
    T332077086-22-7
    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.
    • $32
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  • Lanicemine dihydrochloride
    T60471153322-06-6In house
    Lanicemine dihydrochloride (AZD-6765 dihydrochloride) is a low-capture NMDA channel blocker with antidepressant activity and can be used to study neurological diseases.
    • $30
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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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  • 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 improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.
    • $350
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  • NMDA
    T66086384-92-5
    N-Methyl-D-aspartic acid is an amino acid that, as the D-isomer, is the defining agonist for the NMDA (N-Methyl-D-aspartic acid) receptor subtype of glutamate receptors.
    • $35
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  • Ibotenic acid
    TQ02792552-55-8
    Ibotenic acid (RS-42358-197) has agonist activity at both the NMDA and trans-ACPD or metabotropic quisqualate receptors.
    • $40
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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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  • DL-AP5
    T2273376326-31-3
    DL-AP5 is the racemic form of a selective N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant effects.
    • $30
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  • Riluzole
    T03491744-22-5
    Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
    • $45
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  • Neboglamine hydrochloride
    T606122759182-59-5In house
    Neboglamine (CR-2249, XY-2401) hydrochloride, an orally active positive modulator of the NMDA receptor glycine site, can be used in schizophrenia research [1].
    • $227 TargetMol
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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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  • Transcrocetinate disodium
    TQ0027591230-99-8
    Transcrocetinate disodium (Disodium trans-crocetinate), extracted from saffron (Crocus sativus L.), is a high-affinity antagonist of NMDA receptor.
    • $32
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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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  • 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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  • Radiprodil
    T5385496054-87-6
    Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).
    • $41
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  • Quinolinic acid
    T409689-00-9
    Quinolinic acid (QUIN) is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway.
    • $41
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  • Cycloleucine
    T962652-52-8
    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.
    • $39
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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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  • NS-102
    T38779136623-01-3In house
    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.
    • $158 TargetMol
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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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  • Flutriafol
    T786776674-21-0
    Flutriafol is a pesticide, demethylation inhibitor, and NMDA receptor agonist
    • $39
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  • Memantine hydrochloride
    T144341100-52-1
    Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.
    • $42
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  • Felbamate
    T194625451-15-4
    Felbamate (W-554) is an Anti-epileptic Agent. The physiologic effect of felbamate is by means of Decreased Central Nervous System Disorganized Electrical Activity.
    • $35
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  • Urethane
    T005151-79-6
    Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.
    • $29
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  • Pregnenolone monosulfate
    T125361247-64-9
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a potent nootropic steroid that positively regulates NMDA recordings and is utilized in the study of neuroticism and depression.
    • $46
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  • Ro 25-6981 Maleate
    T12758L1312991-76-6
    Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptor blocker, specifically targeting the NR2B subunit (IC50 values are 0.009 μM for NR1C NR2B and 52 μM for NR1C NR2A receptor subunit combinations).
    • $34
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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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  • 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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  • 1-Aminocyclopropane-1-carboxylic acid
    T475222059-21-8
    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.
    • $46
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  • Procyclidine hydrochloride
    T49791508-76-5
    Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) is a potent anticholinergic agent and also have NMDA antagonist properties.
    • $289
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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.
    • $112
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  • Orphenadrine hydrochloride
    T1308341-69-5
    Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
    • $29
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  • Ifenprodil Tartrate
    T118623210-58-4
    Ifenprodil is a selective NMDA receptor (glutamate) antagonist.
    • $50
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  • O-Phospho-L-serine
    T1324407-41-0
    O-Phospho-L-serine (Phosphoserine) is the phosphoric acid ester of serine.
    • $33
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  • Procaine hydrochloride
    T080251-05-8
    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.
    • $31
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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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  • 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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  • Flupirtine maleate
    T650475507-68-5
    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.
    • $45
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  • UBP551
    T835189-35-0
    UBP551 is a potent and selective NMDA receptors modulator.
    • $30
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  • D-Serine
    T8394312-84-5
    D-Serine ((R)-Serine), an endogenous amino acid, is a potent co-agonist at the NMDA glutamate receptor.
    • $30
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