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Membrane transporter/Ion channel

Monoamine Transporter

(16)

Monocarboxylate transporter

Na-K-Cl cotransporter

Sodium-dependent phosphate transporter

Neuroscience

AAK1 (AP2 associated kinase 1)

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(47)

iGluR

(118)

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

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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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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Dizocilpine

T625977086-21-6

MK-801 (Dizocilpine (MK-801)) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

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D-AP5

T1093079055-68-8

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

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NBQX

T4113118876-58-7

NBQX (FG9202) is a potent, selective and competitive AMPA receptor antagonist. Neuroprotective and anticonvulsant; active in vivo.

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Dizocilpine Maleate

T332077086-22-7

Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.

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Caroverine hydrochloride

T913355750-05-5

Caroverine hydrochloride (Caroverine HCL) is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. It is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action, and can be used for the research of inner ear tinnitus.

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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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UK-240455

T13248178908-09-3In house

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.

$350

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SYM 2081

T1696331137-74-3

SYM 2081 is a specific kainate receptor agonist with an IC50 value of 35 nM for [3H]-kainate binding. SYM 2081 depolarizes the muscle and reduces the EPSP amplitude.

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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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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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Radiprodil

T5385496054-87-6

Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

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AMPA receptor modulator-1

T103072036074-41-4In house

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

$117

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YM90K

T8435154164-30-4

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

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JNJ-61432059

T156232035814-50-5

JNJ-61432059 is an orally active and selective negative modulator of TARP γ-8 selective AMPAR (pIC50: 9.7).

$113

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CNQX

T7178115066-14-3

CNQX (FG9065) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively)

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Tat-NR2B9c

T13112500992-11-0

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

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PEAQX tetrasodium hydrate

T16451

PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A 2A was 270 nM and 29600 nM against hNMDAR 1A 2B, respectively.

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Memantine hydrochloride

T144341100-52-1

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

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CX546

T7580215923-54-9

CX546 is an AMPA receptor modulator. CX546 enhances cognitive function in rats. It has also been proposed as a treatment for schizophrenia.

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Sepimostat

T8920103926-64-3

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

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Rapastinel Trifluoroacetate

T58191435786-04-1

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.

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Flupirtine maleate

T650475507-68-5

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

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Ifenprodil Tartrate

T118623210-58-4

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

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Orphenadrine hydrochloride

T1308341-69-5

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

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Isoxsuprine hydrochloride

T0324579-56-6

Isoxsuprine hydrochloride (Isolait) is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle.

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Philanthotoxin 74 dihydrochloride

T165241227301-51-0

Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.

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TAK-653

T615181358751-06-0

TAK-653, a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.

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Naspm trihydrochloride

T12187L1049731-36-3

Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride) is a synthetic analogue of Joro spider toxin and acts as an antagonist of calcium-permeable AMPA (CP-AMPA) receptors.

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DNQX

T73042379-57-9

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

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CNQX disodium

T8458479347-85-8

CNQX disodium is a competitive non-NMDA receptor antagonist and competitive AMPA/kainate receptor antagonist in neuronal cultures.

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CP 465022

T21584199655-36-2

CP 465022 hydrochloride is a potent, and selective noncompetitive antagonist of AMPA receptor with anticonvulsant activity. CP 465022 hydrochloride inhibits Kainate-induced response with an IC50 of 25 nM in rat cortical neurons.

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Procyclidine hydrochloride

T49791508-76-5

Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) is a potent anticholinergic agent and also have NMDA antagonist properties.

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MDL-29951

T1897130798-51-5

MDL-29951 is a novel glycine antagonist for NMDA receptor activation.

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(-)-Huperzine A

T3026102518-79-6

(-)-Huperzine A (HupA) , an active Lycopodium alkaloid extracted from the traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

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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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Piracetam

T04267491-74-9

Piracetam (UCB-6215), a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), is used in therapy of the extensive cognitive disorders.

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Mibampator

T15820375345-95-2

Mibampator (LY451395) is an effective and selective AMPA receptor potentiator.

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NMDAR antagonist 1

T55222220162-06-9

NMDAR antagonist 1 is an orally active, NR2B-selective NMDAR antagonist.

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NMDAR/TRPM4-IN-2

T726622243506-33-2

NMDAR/TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR/TRPM4 interaction.NMDAR/TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.NMDAR/TRPM4-IN-2 has neuroprotective activity against NMDA-induced hippocampal neuronal cell death and mitochondrial dysfunction. NMDAR/TRPM4-IN-2 showed neuroprotective activity against NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons with an IC50 value of 2.1 μM.

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Omberacetam

T7108157115-85-0

Omberacetam (Noopept) is a synthetic dipeptide that has been shown to produce positive nootropic and cognitive effects in animal models by a mechanism similar to other related racetam compounds.

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Topiramate

T067597240-79-4

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications.

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TCN 201

T7870852918-02-6

TCN 201 is a selective antagonist of NMDA receptors containing the NR2A subunit.

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1-Aminocyclobutanecarboxylic acid

T2254222264-50-2

1-Aminocyclobutanecarboxylic acid (ACBC) is a NMDA receptor partial agonist. 1-Aminocyclobutanecarboxylic acid act at the glycine site, NR1[1].

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PEAQX

T4171459836-30-7

PEAQX (NVP-AAM077)(NVP-AAM 077) is an effective and orally available NMDA antagonist. It can inhibit human NMDA receptors for 1A/2A(IC50: 270 nM), rather than 1A/2B(29, 600 nM).

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Orphenadrine Citrate

T66184682-36-4

Orphenadrine Citrate (Flexon) is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.

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