Overview
GYKI 52466 hydrochloride (#G-125) is a highly pure, synthetic, and biologically active compound.
Structure
For research purposes only, not for human use
Applications
Citations (1)
Citations
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Properties
Technical Specifications
MW 329.78
Purity >96.6%
Molecular formula C17H16ClN3O2.
Form Lyophilized powder.
CAS No. 192065-56-8
Source Synthetic
Chemical name 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride.
Biological Activity
Target AMPA/Kainate receptors
Effective concentration 300 nM - 300 µM.
Activity GYKI 52466 is a selective allosteric AMPA/kainate receptor antagonist, with an IC50 of ~10 μM for AMPA induced currents in cultured superior colliculus neurons1.
References
- Rammes, G. et al. (1996) Br. J. Pharmacol. 117, 1209.
Solubility and Storage
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility 30 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Scientific Background
References
Scientific background GYKI 52466 hydrochloride is a non-competitive AMPA and kainate receptor antagonist. It blocks GluK3 homomeric receptors with an IC50 of 63 μM and GluK2b(R)/GluK3 heteroreceptors with an IC50 of 32 μM at high concentrations. GYKI 52466 has been reported to prevent the excitotoxic action of high extracellular glutamate levels due to its potent non-competitive AMPA receptor antagonistic effect. It has been demonstrated histologically that GYKI 52466 has neuroprotective actions in experimental models of global and focal cerebral ischaemia. The compound was widely investigated in experimental seizure models, where it provided effective protection against convulsions evoked by chemical agents such as AMPA or kainate, electroshock and audiogenic stimulation1.
References
- Szabados, T. et al. (2001) Brain Res. Bull. 55, 387.
Last Update: 08/01/2025
