GYKI 52466

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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.

For research use only. We do not sell to patients.

GYKI 52466 Chemical Structure

CAS No. : 102771-26-6

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Other Forms of GYKI 52466:

GYKI 52466 dihydrochloride Get quote
GYKI 52466 hydrochloride Get quote

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Kainate Receptor

11 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Neuron	IC₅₀	10.8 μM Compound: GYKI-52466	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	[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

GYKI 52466 (intraperitoneal injection; 1.76-13.2 mg/kg; once) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female DBA/2 mice tested for sound-induced seizure responses^[2]
Dosage:	1.76-13.2 mg/kg
Administration:	Intraperitoneal injection; 1.76-13.2 mg/kg; once
Result:	Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).

Molecular Weight

293.32

Formula

C₁₇H₁₅N₃O₂

CAS No.

102771-26-6

SMILES

NC1=CC=C(C2=NN=C(C)CC3=CC4=C(OCO4)C=C32)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

GYKI 52466 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GYKI 52466102771-26-6GYKI52466GYKI-52466iGluRIonotropic glutamate receptorskainateAMPAneurological disordersParkinson's diseasecultured rat hippocampal neuronsInhibitorinhibitorinhibit

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