1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. GYKI 52466 dihydrochloride

GYKI 52466 dihydrochloride 

Cat. No.: HY-103234A
Handling Instructions

GYKI 52466 dihydrochloride is a potent, selective, orally active and non-competitive kainate- and AMPA-activated currents antagonist with IC50s of 7.5 μM and 11 μM, respectively. GYKI 52466 dihydrochloride is inactive against N-methyl-D-aspartate (NMDA) or γ-aminobutyric acid responses. GYKI 52466 dihydrochloride ia a muscle relaxant and anticonvulsant agent, and has good blood brain barrier permeability.

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

GYKI 52466 dihydrochloride Chemical Structure

GYKI 52466 dihydrochloride Chemical Structure

CAS No. : 2319722-40-0

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Description

GYKI 52466 dihydrochloride is a potent, selective, orally active and non-competitive kainate- and AMPA-activated currents antagonist with IC50s of 7.5 μM and 11 μM, respectively. GYKI 52466 dihydrochloride is inactive against N-methyl-D-aspartate (NMDA) or γ-aminobutyric acid responses. GYKI 52466 dihydrochloride ia a muscle relaxant and anticonvulsant agent, and has good blood brain barrier permeability[1][2].

IC50 & Target

IC50: 7.5 μM (Kainate receptor) and 11 μM (AMPA receptor)[1]

In Vitro

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. GYKI 52466 also suppresses non-NMDA receptor-mediated spontaneous synaptic currents via a postsynaptic action[1].

In Vivo

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.)[2].
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[2].

Animal Model: Male and female DBA/2 mice (3-4-week-old) induced sound[2]
Dosage: 1.76-13.2 mg/kg (6-45 μmol/kg)
Administration: Intraperitoneal injection; once
Result: Provided potent anticonvulsant protection against sound-induced seizures in seizure-susceptible DBA/2 mice.
Molecular Weight

366.24

Formula

C₁₇H₁₇Cl₂N₃O₂

CAS No.

2319722-40-0

SMILES

NC1=CC=C(C2=NN=C(C)CC3=CC4=C(OCO4)C=C32)C=C1.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

GYKI 52466GYKI52466GYKI-52466iGluRIonotropic glutamate receptorsAMPAkainatenoncompetitivenon-NMDAmusclerelaxantanticonvulsantglutamateBBBInhibitorinhibitorinhibit

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GYKI 52466 dihydrochloride
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HY-103234A
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