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

iGluR

Ionotropic glutamate receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-183101
    AMPAR modulator-12
    Modulator
    AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression.
    AMPAR modulator-12
  • HY-179108
    NMDAR modulator 1
    Modulator
    NMDAR modulator 1 (Compound 12) is a positive, allosteric GluN1/GluN2B receptor modulator. NMDAR modulator 1 enhances NMDAR current. NMDAR modulator 1 can be used in the research of psychiatric disorders.
    NMDAR modulator 1
  • HY-120074
    UBP512
    Modulator
    UBP512 is an NMDA receptor modulator with the activity to regulate NMDA receptor activity. UBP512 is a GluN2A-selective enhancer and GluN2C and GluN2D inhibitor, belonging to a new generation of NMDA receptor modulators, which may have potential effects on the study and inhibition of related neurological diseases.
    UBP512
  • HY-15786
    SGE-201
    Modulator
    SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.
    SGE-201
  • HY-B0585S1
    Piracetam-d6
    Modulator
    Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
    Piracetam-d<sub>6</sub>
  • HY-155628
    AMPA receptor modulator-6
    Modulator
    AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases.
    AMPA receptor modulator-6
  • HY-16728A
    Rapastinel acetate
    Modulator
    Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.
    Rapastinel acetate
  • HY-145370
    GluN2B receptor modulator-1
    Modulator
    GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
    GluN2B receptor modulator-1
  • HY-182631
    CX1763
    Modulator
    CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression.
    CX1763
  • HY-186183
    Normethyl-ZCAN262
    Modulator
    Normethyl-ZCAN262 (Normethyl-262) is a blood-brain barrier-permeable selective GluR2/AMPAR receptor modulator. Normethyl-ZCAN262 inhibits AMPA-mediated neurotoxicity, the formation of the GAPDH-GluR2 complex, and GluR2/AMPAR neurotoxicity. Normethyl-ZCAN262 enables in vivo imaging of brain AMPA receptors and is used in research related to multiple sclerosis, amyotrophic lateral sclerosis, neuroinflammation, stroke, epilepsy, Parkinson's disease, Alzheimer's disease, dementia, and Huntington's disease.
    Normethyl-ZCAN262
  • HY-181127
    GluN2B-NMDAR Allosteric modulator 1
    Modulator
    GluN2B-NMDAR Allosteric modulator 1 is a selective GluN2B-NMDAR positive allosteric modulator. GluN2B-NMDAR Allosteric modulator 1 can increase glutamate- and aspartate-evoked GluN2B-NMDAR-gated currents with EC50 values of 43.7 and 18 nM. GluN2B-NMDAR Allosteric modulator 1 can reverse anxiety-like behavior and social cognition deficits in mice. GluN2B-NMDAR Allosteric modulator 1 can be used for the research of neurological disease, such as anxiety.
    GluN2B-NMDAR Allosteric modulator 1
  • HY-168966
    JNJ-54082730
    Modulator
    JNJ-54082730 (Compound 1) is the orally active inhibitor for phosphodiesterase (PDE) that inhibits PDE2A, PDE3B, and PDE10A2 with IC50s of 0.95 nM, 6.17 μM (pIC50=5.21) and 87.1 nM (pIC50=7.06), respectively. JNJ-54082730 modulates the activity of AMPA receptor, enhance the synaptic plasticity and promotes the learning and memory function in rats models. JNJ-54082730 can cross blood-brain barrier.
    JNJ-54082730
  • HY-120155
    MS-377
    Modulator
    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-124906
    JAMI1001A
    Modulator
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
    JAMI1001A
  • 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-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-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-101363R
    1-BCP (Standard)
    Modulator
    1-BCP (Standard) is the analytical standard of 1-BCP. This product is intended for research and analytical applications. 1-BCP (Piperonylic acid piperidide) is a centrally active agent that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
    1-BCP (Standard)
  • HY-101216R
    Org-26576 (Standard)
    Modulator
    Org-26576 (Standard) is the analytical standard of Org-26576 (HY-101216). This product is intended for research and analytical applications. Org-26576 is a AMPA receptor positive allosteric modulator.
    Org-26576 (Standard)
  • HY-160931
    NMDA receptor modulator 8
    Modulator
    NMDA receptor modulator 8 (Compound 3-6) is a modulator for NMDA receptor, with 50%-100% potentiation of NMDA receptor at 10 μM.
    NMDA receptor modulator 8
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