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rat NMDA receptors

" in MedChemExpress (MCE) Product Catalog:

26

Inhibitors & Agonists

1

Natural
Products

Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-15084
    Dizocilpine maleate
    Maximum Cited Publications
    44 Publications Verification

    (+)-MK 801 Maleate

    		 iGluR Neurological Disease
    Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
    Dizocilpine maleate
  • HY-15084B
    Dizocilpine
    Maximum Cited Publications
    44 Publications Verification

    MK-801

    		 iGluR Neurological Disease
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
    Dizocilpine
  • HY-100834
    5,7-Dichlorokynurenic acid
    1 Publications Verification

    5,7-DCKA

    		 iGluR Neurological Disease
    5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
    5,7-Dichlorokynurenic acid
  • HY-18698
    L-701324

    		iGluR Neurological Disease
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
    L-701324
  • HY-157959
    Orphenadrine

    (±)-Orphenadrine

    		 iGluR Cytochrome P450 Cholinesterase (ChE) Neurological Disease Cancer
    Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
    Orphenadrine
  • HY-125931
    Unifiram

    DM232

    		 iGluR Neurological Disease Inflammation/Immunology
    Unifiram (DM232) is a AMPA receptor activator and cognitive enhancer. Unifiram activates the AMPA-mediated neurotransmission system. Unifiram reverses NBQX-induced amnesia in the passive avoidance test in mice. Unifiram reverses the antagonistic effect of kynurenic acid on NMDA-mediated [ 3H]NA release in rat hippocampal slices. Unifiram enhances excitatory synaptic transmission in the rat hippocampus in vitro. Unifiram can be used in studies related to amnesia and cognitive dysfunction, including age-related memory decline, neurodegenerative diseases such as Alzheimer's disease or Parkinson's disease, multiple sclerosis, schizophrenia, and attention deficit hyperactivity disorder .
    Unifiram
  • HY-14840
    Phenylpiracetam

    Carphedon

    		 nAChR Dopamine Transporter GABA Receptor iGluR Neurological Disease
    Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC50 of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress .
    Phenylpiracetam
  • HY-N2125
    Parishin C

    		5-HT Receptor iGluR Caspase Interleukin Related TNF Receptor SOD NF-κB Neurological Disease Inflammation/Immunology
    Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC50 of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis .
    Parishin C
  • HY-107520
    MNI-caged-L-glutamate

    		Drug Derivative Neurological Disease
    MNI-caged-L-glutamate is an inert photolabile glutamate precursor. MNI-caged-L-glutamate does not modulate NMDA and AMPA receptor function in cultured neurones. MNI-caged-L-glutamate can be used for research on neurotransmitters .
    MNI-caged-L-glutamate
  • HY-W073501
    trans-Glutaconic acid

    trans-2-Pentenedioic acid

    		 Drug Isomer Endogenous Metabolite Cardiovascular Disease Metabolic Disease
    trans-Glutaconic acid (trans-2-Pentenedioic acid) is the trans isomer of Glutaconic acid (HY-W073501A). trans-Glutaconic acid is a neurotoxic metabolite. trans-Glutaconic acid induces weak neurotoxicity in cultured cerebral neocortical neurons. trans-Glutaconic acid elicits significant electrophysiological responses in rat neocortical wedge preparations at high concentrations. trans-Glutaconic acid can be used in studies related to glutaric acidemia type 1 .
    trans-Glutaconic acid
  • HY-103344
    ZJ43

    		Aminopeptidase Carboxypeptidase mGluR Neurological Disease
    ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC50 of 2.4 nM and Ki of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury .
    ZJ43
  • HY-172419
    Blixeprodil

    GM-1020

    		 iGluR Neurological Disease
    Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression .
    Blixeprodil
  • HY-114753
    Neboglamine

    CR-2249; XY-2401

    		 iGluR Neurological Disease
    Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .
    Neboglamine
  • HY-120155
    MS-377

    		Sigma Receptor iGluR Neurological Disease
    MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia .
    MS-377
  • HY-171979
    Fluorolintane

    		iGluR Neurological Disease
    Fluorolintane exhibits high affinity for N-methyl-D-aspartate (NMDA) receptors with a Ki of 87.92 nM. Fluorolintane inhibits prepulse inhibition in rats. Fluorolintane also inhibits NMDA receptor-induced field excitatory postsynaptic potentials in rat hippocampal slices .
    Fluorolintane
  • HY-19225
    Ensaculin

    KA-672 hydrochloride; Anseculin hydrochloride

    		 iGluR Neurological Disease
    Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems .
    Ensaculin
  • HY-105353
    CEB-1604

    		iGluR Neurological Disease
    CEB-1604 is an NMDA receptor antagonist. CEB-1604 inhibits NMDA-induced currents in oocytes transfected with NMDA receptor isoforms (NR1/NR2A, NR1/NR2B, NR1/NR2C, NR1/NR2D) with IC50 values ranging from 5 to 12 μM. CEB-1604 abolishes NMDA-dependent epileptiform discharges in rat cortical wedge preparations and reduces the depolarizing effects of NMDA. CEB-1604 can be used in the research field of neurological damage diseases .
    CEB-1604
  • HY-121704
    SR 57227A free base

    		iGluR Neurological Disease
    SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.
    SR 57227A free base
  • HY-116142
    CP-283097

    		iGluR Neurological Disease
    CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
    CP-283097
  • HY-100834A
    5,7-Dichlorokynurenic acid sodium

    5,7-DCKA sodium

    		 iGluR Neurological Disease
    5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
    5,7-Dichlorokynurenic acid sodium
  • HY-105693
    Fluorofelbamate

    		iGluR Neurological Disease
    Fluorofelbamate, a Felbamate (HY-B0184) analog, is a potent NMDA receptor antagonist. Fluorofelbamate exhibits anticonvulsant and antiepileptogenic effects in an experimental rat model of self-sustaining status epilepticus (SSSE). Fluorofelbamate can be used for epilepsy research .
    Fluorofelbamate
  • HY-131691
    NMDAR blocker 1

    		iGluR Calcium Channel Neurological Disease
    NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca 2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases .
    NMDAR blocker 1
  • HY-156505A
    R-(+)-EU-1180-453

    		iGluR Neurological Disease
    R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain .
    R-(+)-EU-1180-453
  • HY-182479
    MDL 100748

    		iGluR Others Neurological Disease
    MDL 100748 is an NMDA receptor glycine site antagonist. MDL 100748 modulates NMDA receptor function by acting at the strychnine-insensitive glycine site, which is required for NMDA receptor activation alongside glutamate. MDL 100748 decreases response rates in operant conditioning sessions in phencyclidin (PCP)-trained rats. MDL 100748 can be used for reserach on dementias and schizophrenia .
    MDL 100748
  • HY-120681
    CGP39653

    		iGluR Neurological Disease
    CGP39653 is a competitive NMDA receptor antagonist that inhibits receptor function by competing with glutamate for the binding site .
    CGP39653
  • HY-126939
    MN-05

    		Reactive Oxygen Species (ROS) Calcium Channel iGluR Neurological Disease
    MN-05 is a dual neuroprotective and vasodilatory NMDA receptor inhibitor.MN-05 blocks calcium influx, reduces free radical production, and maintains mitochondrial membrane potential in cortical neurons exposed to glutamate.MN-05 dilates aortic rings against phenylephrine-induced contraction.MN-05 protects neurons against glutamate-induced injury in vitro.MN-05 can be used for the research of neurodegenerative diseases .
    MN-05

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