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.


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TRANS-1-AMINOCYCLOBUTANE-1,3-DICARBOXYLIC ACID

trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission[1].

  • CAS Number: 117488-23-0
  • MF: C6H9NO4
  • MW: 159.14000
  • Catalog: iGluR
  • Density: 1.568g/cm3
  • Boiling Point: 288.1ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 128ºC

LY 392098

LY 392098 is a selective, potent and centrally active positive allosteric modulator of AMPAR; enhances glutamate (100 uM) stimulated ion influx through recombinant homomeric human AMPAR ion channels with EC50 of 1.77 uM (GluR1(i)), 0.22 uM (GluR2(i)), 0.56 uM (GluR2(o)), 1.89 uM (GluR3(i)) and 0.20 uM (GluR4(i); enhances a dose-dependent manner responses to AMPA, potentiates the synaptic excitation of dentate granule cells following perforant path stimulation in vivo.

  • CAS Number: 211311-39-6
  • MF: C18H22FNO2S
  • MW: 335.44
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Decanoic acid-d19

Decanoic acid-d19 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].

  • CAS Number: 88170-22-3
  • MF: C10HD19O2
  • MW: 191.38200
  • Catalog: iGluR
  • Density: 0.991 g/mL at 25ºC
  • Boiling Point: 268-270ºC(lit.)
  • Melting Point: 30-32ºC(lit.)
  • Flash Point: N/A

7-Chlorokynurenic acid sodium salt

7-Chlorokynurenic acid sodium salt is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM.

  • CAS Number: 1263094-00-3
  • MF: C10H5ClNNaO3
  • MW: 245.594
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sepimostat

Sepimostat exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM[1].

  • CAS Number: 103926-64-3
  • MF: C21H19N5O2
  • MW: 373.40800
  • Catalog: iGluR
  • Density: 1.39g/cm3
  • Boiling Point: 607.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 321.2ºC

UBP141

UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice[1][2].

  • CAS Number: 344768-30-5
  • MF: C21H18N2O5
  • MW: 378.38
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Salfaprodil

Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death[1][2].

  • CAS Number: 916214-57-8
  • MF: C15H7F7KNO3
  • MW: 421.31
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NMDAR/TRPM4-IN-2

NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].

  • CAS Number: 2243506-33-2
  • MF: C11H19BrCl2N2
  • MW: 330.09
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CP465022 HCl

CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].

  • CAS Number: 199655-36-2
  • MF: C26H24ClFN4O
  • MW: 462.95
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Methoxy-6-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propoxy}-3,4-dimethyl-2H-chromen-2-one

Ensaculin free base (KA-672) is a NMDA antagonist and have high affinities to serotonergic 5-HT1A and 5-HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems[1].

  • CAS Number: 155773-59-4
  • MF: C26H32N2O5
  • MW: 452.54
  • Catalog: 5-HT Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 632.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 336.0±31.5 °C

N-Methyl-D-aspartic acid

NMDA is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.

  • CAS Number: 6384-92-5
  • MF: C5H9NO4
  • MW: 147.129
  • Catalog: iGluR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 258.2±30.0 °C at 760 mmHg
  • Melting Point: 187-192 °C
  • Flash Point: 110.0±24.6 °C