GYKI 52466
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
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- CAS No.: 102771-26-6
- Formule: C17H15N3O2
- Masse moléculaire:293.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
Other In-stock Forms of GYKI 52466
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Kainate Receptor 11 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Neuron | IC50 |
10.8 μM
Compound: GYKI-52466
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Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
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[PMID: 18083036] |
In Vitro
GYKI 52466 (0.3-100 μM) inhibits inward currents activated by AMPA and Kainate receptor in cultured rat hippocampal neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female DBA/2 mice tested for sound-induced seizure responses[2]
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Dosage:1.76-13.2 mg/kg
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Administration:Intraperitoneal injection; 1.76-13.2 mg/kg; once
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Result:Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).
Chemical Information
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CAS No. 102771-26-6
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Masse moléculaire 293.32
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Formule C17H15N3O2
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SMILES
NC1=CC=C(C2=NN=C(C)CC3=CC4=C(OCO4)C=C32)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. S D Donevan, et al. GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron. 1993 Jan;10(1):51-9. [Content Brief]
[2]. A G Chapman, et al. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res. 1991 Jul;9(2):92-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GYKI 52466 Related Classifications
HY-103234 Related Classifications
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