Overview
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- Perrais, D. et al. (2009) Neuropharmacology 56, 131.
- Szabados, T. et al. (2001) Brain. Res. Bull. 55, 387.
It is recommended to aliquot stock solutions to prevent repeated thawing.
Alomone Labs GYKI 53655 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes.Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 50 µM GYKI 53655 hydrochloride (#G-220), as indicated (bar), at a holding potential of -80 mV.
GYKI 53655 hydrochloride, a racemic 2,3-benzodiazepine is a AMPA and Kainate receptor antagonist. It acts as a non-competitive antagonist and negative allosteric modulator of AMPA receptors and is selective over Kainate receptors. It inhibits AMPA mediated responses in recombinant human GluA1 receptors expressed in HEK293 cells with an approximate IC50 values of 6 µM, and in recombinant human GluA4 expressing cells with an approximate IC50 values of 5 µM1. GYKI 53655 have been reported to be therapeutically effective in several animal models of epilepsy and global brain ischaemia1.
The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors that mediate fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity, learning, and memory1,2.
Kainate receptors are highly expressed in the developing brain, where they are tonically activated to modulate synaptic transmission, network excitability, and synaptogenesis3.
