2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. iGluR

iGluR

Ionotropic glutamate receptors

iGluR

Related Products

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iGluR (ionotropic glutamate receptor) is a ligand-gated ion channel that is activated by the neurotransmitter glutamate. iGluR are integral membrane proteins compose of four large subunits that form a central ion channel pore. Sequence similarity among all known glutamate receptor subunits, including the AMPA, kainate, NMDA, and δ receptors.

AMPA receptors are the main charge carriers during basal transmission, permitting influx of sodium ions to depolarise the postsynaptic membrane. NMDA receptors are blocked by magnesium ions and therefore only permit ion flux following prior depolarisation. This enables them to act as coincidence detectors for synaptic plasticity. Calcium influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.

iGluR Isoform Specific Products:

iGluR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-168771
    gamma-DGG TFA
    		Antagonist 99.95%
    gamma-DGG TFA is the antagonist for excitatory amino acid, that blocks NMDA-(HY-17551), Kainate-(HY-N2309) and Quisqualate-(HY-12597) induced depolarization, and antagonises the excitatory postsynaptic potential (e.p.s.p.) in rat hippocampal slices.
    gamma-DGG TFA
  • HY-145897
    NMDA-IN-2
    		Inhibitor
    NMDA-IN-2 (compound 6b), a Procaine derivative, is a NMDA receptor 2B subtype inhibitor.
    NMDA-IN-2
  • HY-15787
    SGE-301
    		Modulator
    SGE-301 is a positive, allosteric NMDAR modulator. SGE-301 recovers NMDAR density and long-term potentiation to normal values. SGE-301 can be used in the research of neurological disorders.
    SGE-301
  • HY-100616A
    trans-ACBD
    		Agonist
    trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission.
    trans-ACBD
  • HY-138973
    Neramexane
    		Antagonist
    Neramexane is an oral N-methyl-D-aspartate (NMDA) receptor antagonist, as a potential neuroprotectant for various central nervous system disorders, including Alzheimer's disease, and for the potential treatment of drug and alcohol dependence, and pain.
    Neramexane
  • HY-173398
    NMDAR antagonist 5
    		Antagonist
    NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression.
    NMDAR antagonist 5
  • HY-170898
    Antidepressant agent 8
    		Antagonist
    Antidepressant agent 8 (Compound 1f) is a selective antagonist for the NMDA receptor GluN1/2A with an IC50 of 2.94 μmol/L. Antidepressant agent 8 exhibits antidepressant-like effects in Hydrocortisone (HY-N0583)-induced zebrafish depression model. Antidepressant agent 8 can cross blood-brain barrier.
    Antidepressant agent 8
  • HY-116205
    UBP684
    UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
    UBP684
  • HY-19858
    LY-466195
    		Antagonist
    LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively.
    LY-466195
  • HY-164264
    Caged MK801
    		Inhibitor
    Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible.
    Caged MK801
  • HY-106408AR
    Nelonemdaz potassium (Standard)
    		Antagonist
    Nelonemdaz potassium (Standard) is the analytical standard of Nelonemdaz potassium (HY-106408A). This product is intended for research and analytical applications. Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death.
    Nelonemdaz potassium (Standard)
  • HY-108235AR
    Lanicemine dihydrochloride (Standard)
    		Antagonist
    Lanicemine dihydrochloride (Standard) is the analytical standard of Lanicemine (dihydrochloride) (HY-108235A). This product is intended for research and analytical applications. Lanicemine (AZD6765) dihydrochloride is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.
    Lanicemine dihydrochloride (Standard)
  • HY-10932R
    Aniracetam (Standard)
    		Modulator
    Aniracetam (Standard) is the analytical standard of Aniracetam. This product is intended for research and analytical applications. Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.
    Aniracetam (Standard)
  • HY-100811AR
    7-Chlorokynurenic acid sodium salt (Standard)
    		Antagonist
    7-Chlorokynurenic acid (sodium salt) (Standard) is the analytical standard of 7-Chlorokynurenic acid (sodium salt). This product is intended for research and analytical applications. 7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid sodium salt is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid sodium salt has potent antinociceptive actions after neuraxial delivery.
    7-Chlorokynurenic acid sodium salt (Standard)
  • HY-N2370R
    24-Hydroxycholesterol (Standard)
    		Activator
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
    24-Hydroxycholesterol (Standard)
  • HY-129517
    UBP714
    		Agonist
    UBP714 exhibts agonistic activity for recombinant GluN1/GluN2 receptor by binding to the positive allosteric site (PAM) of NMDARs. UBP714 enhances NMDAR-mediated field excitatory postsynaptic potentials (f-EPSPs) in Xenopus oocytes .
    UBP714
  • HY-B0184A
    Felbamate hydrate
    		Inhibitor
    Felbamate hydrate (W-554 hydrate) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
    Felbamate hydrate
  • HY-W017500R
    N-Methyl-DL-aspartic acid (Standard)
    		Agonist
    N-Methyl-DL-aspartic acid is a glutamate analogue and a NMDA receptor agonist and can be used for neurological diseases research.
    N-Methyl-DL-aspartic acid (Standard)
  • HY-204630
    NMDAR modulator 2
    		Modulator
    NMDAR modulator 2 (comound 9062) is a NMDA receptor modulator that is modulator of NMDA receptor function. NMDAR modulator 2 can be used for the study of psychiatric disorders in which glutamatergic transmission is pathologically increased (e.g., treatment resistant depression).
    NMDAR modulator 2
  • HY-90003S
    Tianeptine-d12
    		Agonist
    Tianeptine-d12 is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine-d<sub>12</sub>
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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