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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.

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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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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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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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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D-AP5
T1093079055-68-8
D-AP5 (D-APV) is an NMDA receptor antagonist.
  • $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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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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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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R-(+)-EU-1180-453
T696112488764-06-1In house
R-(+)-EU-1180-453 is a novel GluN2C D selective NMDAR-positive modulator for the study of neurological disorders.
  • $1,970
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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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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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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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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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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.
  • $38
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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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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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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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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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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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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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Flutriafol
T786776674-21-0
Flutriafol is a pesticide, demethylation inhibitor, and NMDA receptor agonist
  • $39
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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.
  • $88
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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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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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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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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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GNE-8324
T319811698901-76-6In house
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.
  • $1,520
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Rapastinel Trifluoroacetate
T58191435786-04-1
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.
  • $33
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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.
  • $30
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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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Ifenprodil Tartrate
T118623210-58-4
Ifenprodil is a selective NMDA receptor (glutamate) antagonist.
  • $50
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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.
  • $30
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Spermidine trihydrochloride
T5080334-50-9
Spermidine trihydrochloride (4-Azaoctamethylenediamine trihydrochloride), a natural polyamine, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
  • $30
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Bupivacaine
T0030L38396-39-3
Bupivacaine (AH-250) is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine can be used for the research of chronic pain.
  • $33
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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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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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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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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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Procyclidine hydrochloride
T49791508-76-5
Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) is a potent anticholinergic agent and also have NMDA antagonist properties.
  • $29
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MDL-29951
T1897130798-51-5
MDL-29951 is a novel glycine antagonist for NMDA receptor activation.
  • $43
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TCS 46b
T23449302799-86-6
NR1A/NR2B NMDA receptor antagonist,orally active
  • $39
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