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GYKI 52466 dihydrochloride

Catalog No. T11522 CAS 2319722-40-0

GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and has good blood-brain barrier permeability.

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GYKI 52466 dihydrochloride Chemical Structure

GYKI 52466 dihydrochloride, CAS 2319722-40-0

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2 mg	5 days	$ 64.00

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Description	GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and has good blood-brain barrier permeability.
Targets&IC50	AMPA receptor:11 μM , Kainate receptor:7.5 μM
In vitro	GYKI 52466 also suppresses non-NMDA receptor-mediated spontaneous synaptic currents via a postsynaptic action.In kinetic experiments with kainate as the agonist, the GYKI 52466 binding and unbinding rates were 1.6 x 105 M-1 s-1 and 3.2 s-1, respectively.
In vivo	GYKI 52466 provides potent anticonvulsant protection against AMPA-induced seizures in Swiss mice. Maximal anticonvulsant protection is observed 5-15 min after the i.p. administration of GYKI 52466 in DBA/2 mice. The ED50 values for the protection against AMPA-induced seizures by GYKI 52466 (15 min, i.p.) is 18.5 (11.5-29.5) μmol/kg.GYKI 52466 (1.76-13.2 mg/kg;?male and female DBA/2 mice;?intraperitoneal injection) treatment provides potent anticonvulsant protection against sound-induced seizures in seizure-susceptible DBA/2 mice.?The ED50 value at 15 min for the protection against sound-induced seizures in DBA/2 mice is 13.7 (11.5-16.5) μmol/kg (GYKI 52466, i.p.).

Molecular Weight	366.24
Formula	C17H17Cl2N3O2
CAS No.	2319722-40-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Donevan SD, 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. 2. Chapman AG, et al. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res. 1991 Jul;9(2):92-6.

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Keywords

GYKI 52466 dihydrochloride 2319722-40-0 Others GYKI 52466 GYKI 52466 Dihydrochloride GYKI52466 GYKI-52466 Dihydrochloride GYKI-52466 GYKI52466 Dihydrochloride inhibitor inhibit

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