iGluR
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.
Targets for iGluR
Products for iGluR
- Cat.No. Product Name Information
- GC33701 Orphenadrine hydrochloride A muscarinic acetylcholine receptor antagonist
- GC16562 PEAQX NMDA antagonist
- GC36865 PEAQX tetrasodium hydrate PEAQX (NVP-AAM077) tetrasodium hydrate is a potent, selective and orally active NMDA antagonist, with IC50 values of 270 nM and 29600 nM for hNMDAR 1A/2B and hNMDAR 1A/2B, respectively.
- GC13007 PEPA Novel allosteric potentiator of AMPA receptor desensitization
- GC36876 Perzinfotel Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects.
- GC64929 Pesampator Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM.
- GC14492 PF 4778574 positive allosteric modulator of AMPA receptors
- GC12703 Philanthotoxin 74 Philanthotoxin 74 (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
- GC13469 Piracetam cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA)
- GC65954 Plazinemdor Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system..
- GC30946 Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist.
- GC16776 QNZ 46 NR2C/NR2D-selective NMDA receptor antagonist
- GC14547 Quinolinic acid NMDA agonist
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GC34753
Radiprodil
An NMDA receptor antagonist
- GC33492 Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties.
- GC30835 Rislenemdaz (MK-0657) Rislenemdaz (MK-0657) (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
- GC19310 Ro 25-6981 Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
- GC18410 Ro 25-6981 (maleate) Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).
- GC31039 RPR104632 RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.
- GC13684 S 18986 positive allosteric modulator of AMPA receptors
- GC18118 SDZ 220-581
- GC37612 SDZ 220-581 Ammonium salt SDZ 220-581 Ammonium salt is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7.
- GC16986 SDZ 220-581 hydrochloride NMDA receptor antagonist
- GC61580 Sepimostat Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit.
- GC61570 Sepimostat dimethanesulfonate Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit.
- GC37703 Sunifiram Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam.
- GC16101 SYM 2081 kainate receptor agonist
- GC13728 SYM 2206 AMPA receptor antagonist
- GC64650 TAK-653 TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats.
- GC19346 Talampanel Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED).
-
GC30774
Tat-NR2B9c
Tat-NR2B9c is designed to prevent nitric oxide (NO) production by preventing postsynaptic density protein 95 (PSD-95) binding to N-methyl-D-aspartate (NMDA) receptors and neuronal nitric oxide synthase.
- GC34828 Tat-NR2B9c TFA Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively.
- GC60354 Tat-NR2Baa Tat-NR2BAA is the control peptide of Tat-NR2B9c, inactive.
- GC11585 TCN 237 dihydrochloride TCN 237 dihydrochloride is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
- GC16149 Topiramate An anticonvulsant
- GC50198 Topiramate - d12 Deuterated topiramate
- GC33341 Transcrocetin (trans-Crocetin) Transcrocetin (trans-Crocetin) (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity. Transcrocetin (trans-Crocetin) (trans-Crocetin) is capable of crossing the blood-brain barrier and reach the central nervous system (CNS).
- GC37821 Transcrocetin meglumine salt Transcrocetin meglumine salt, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
- GC32447 Transcrocetinate disodium (Disodium trans-crocetinate) Transcrocetinate disodium (Disodium trans-crocetinate), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
-
GC30839
Traxoprodil
An antagonist of NR2B subunit-containing NMDA receptors
- GC33685 Tulrampator (CX-1632) Tulrampator (CX-1632) (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor).
- GC38446 UBP 302 An antagonist of GluR5 subunit-containing kainate receptors
-
GC70084
UBP301 hydrochloride
UBP301 hydrochloride is an effective selective antagonist of kainate receptors, with IC50 and KD values of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has a selectivity for kainate receptors over AMPA receptors that is 30 times higher. It is a derivative of Willardiine.
- GC31153 UK-240455 UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.
- GC67922 Zelquistinel
- GC16300 ZK 200775 ZK 200775 (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
- GC30818 ZL006 ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
- GC30457 Zonampanel (YM 872) Zonampanel (YM 872) (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.