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Membrane transporter/Ion channel

Monoamine Transporter

(43)

Monocarboxylate transporter

Na-K-Cl cotransporter

Sodium-dependent phosphate transporter

Neuroscience

AAK1 (AP2 associated kinase 1)

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(124)

iGluR

(401)

iGluR

Ionotropic glutamate receptors (iGluRs) are ligand-gated ion channels that are activated by the neurotransmitter glutamate.[1] They mediate the majority of excitatory synaptic transmission throughout the central nervous system and are key players in synaptic plasticity, which is important for learning and memory. iGluRs have been divided into four subtypes on the basis of their ligand binding properties (pharmacology) and sequence similarity: AMPA receptors, kainate receptors, NMDA receptors and delta receptors.

Filter HomeSignaling PathwaysNeuroscience-Membrane transporter/Ion channeliGluR

CNS-5161 hydrochloride

T10852160756-38-7In house

CNS-5161 hydrochloride (CNS 5161A) is a new antagonist of NMDA ion-channel. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

$509

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Corticosterone

T0948L50-22-6

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

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TAK-137

T708801358749-55-9In house

TAK-137 is an AMPA receptor enhancer with antidepressant effects. TAK-137 has the ability to improve cognition and could be used to study schizophrenia.

$293

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GNE-5729

T154082026635-66-3

GNE-5729 is a positive allosteric modulator of NMDAR with the advantage of crossing the blood-brain barrier and being orally available, with EC50 values of 37 nM, 4.7 μM and 9.5 μM for GluN2A, GluN2C and GluN2D, respectively, and can be used for the study of neurological and psychiatric disorders.

$263

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D-AP5

T1093079055-68-8

D-AP5 (D-APV) is an NMDA receptor antagonist.

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Dalzanemdor

T628391629853-48-0In house

Dalzanemdor (SAGE-718) is an NMDA receptor-positive modulator of metabolism that can be used to study Huntington's chorea, Alzheimer's disease, and cognitive dysfunction.

$670

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Transcrocetinate disodium

TQ0027591230-99-8

Transcrocetinate disodium (Disodium trans-crocetinate), extracted from saffron (Crocus sativus L.), is a high-affinity antagonist of NMDA receptor.

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CGP 78608 hydrochloride

T107811135278-54-4In house

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1/GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

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Dasolampanel

T31208503294-13-1In house

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

$762

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GNE-0723

T154071883518-31-7

GNE-0723 is a selective positive allosteric modulator of the NMDA receptor, with an EC50 of 21 nM for GluN2A. It can cross the blood-brain barrier (BBB) and improve outcomes in Dravet syndrome (DS) and Alzheimer's disease (AD).

$457

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NBQX Disodium

T25853479347-86-9

NBQX Disodium (FG9202 disodium) is a highly selective, competitive AMPA receptor antagonist with neuroprotective and anticonvulsant activity. NBQX Disodium is a salt of NBQX. NBQX is a potent and selective AMPA/rhodosinate receptor antagonist that can be used to antagonize the excitatory toxicity of glutamate. It has anticonvulsant effects in rodent models.

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L-Glutamic acid

T2A249756-86-0

L-Glutamic acid is an excitatory amino acid neurotransmitter and a Glutamic acid receptor agonist, including metabolic glutamic acid receptor (mGluR), AMPA receptor, NMDA receptor and KA receptor. L-Glutamic acid has an excitatory effect on the process of DA release from dopaminergic nerve endings. L-Glutamic acid can be used in the research of neurological diseases. L-Glutamic acid acts on ionic and metabolic Glutamic acid receptors.

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Dizocilpine

T625977086-21-6

Dizocilpine (MK-801) is a selective non-competitive NMDA receptor antagonist with a Kd of 37.2 nM that exhibits anticonvulsant effects. It acts by binding to a site within the NMDA-associated ion channel, blocking the flow of Ca²⁺, and is commonly used to establish schizophrenia models.

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Cyclothiazide

T45732259-96-3

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).

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LY382884

T27949211566-75-5In house

LY382884 is a selective and potent GluR5 kainate receptor antagonist with anxiolytic activity.LY382884 blocks blockade of mossy fibre LTP induction.

$748

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DL-AP5

T2273376326-31-3

DL-AP5 is the racemic form of a selective N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant effects.

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Dizocilpine Maleate

T332077086-22-7

Dizocilpine Maleate (MK-801 maleate) is a potent, selective, and non-competitive NMDA receptor antagonist with a Kd value of 37.2 nM. It is commonly used in the treatment of various neurodegenerative diseases in which NMDA receptors may be involved, and can also be used to induce schizophrenia models.

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Delucemine Hydrochloride

T27143186495-99-8In house

Delucemine Hydrochloride (Delucemine) is a polyamine NMDA receptor antagonist used in the study of neurological disorders such as depression and Alzheimer's disease.

$293

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MRZ 2-514

T12110202808-11-5

MRZ 2-514 (8-bromo-4,5-dihydroxypyridazino[4,5-b]quinolin-1-one) is a strychnine-insensitive modulatory site of the NMDA receptor (glycineB)antagonist with Ki of 33 μM.

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Evans blue

T0313314-13-6

Evans blue (C.I. 23860) is an azo dye, inhibits L-glutamate uptake via the membrane-bound excitatory amino acid transporter (EAAT).

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glycine

T2O272856-40-6

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

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CFM-2

T10774178616-26-7In house

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

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GYKI-47261 dihydrochloride

T386011217049-32-5

GYKI-47261 dihydrochloride is an orally active and selective AMPA receptor antagonist, also a CYP2E1 inducer with broad anticonvulsant and neuroprotective activity, used in neurological and cardiovascular research.

$293

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Memantine

T2099319982-08-2

Memantine, an amantadine derivative with some dopaminergic effects, has been proposed as an antiparkinson agent and has may be used to treat moderate to severe Alzheimer's disease. It acts on the glutamatergic system by blocking NMDA receptors.

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