Selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). Skeletal muscle relaxant, orally active anticonvulsant, neuroprotective and anxiolytic in vivo.
Also available in simple stock solutions (ab146716) - add 1 ml of water to get an exact, ready-to-use concentration.
Store at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in 1eq. HCl to 10mM and in DMSO to 25 mM (with heating)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Use at an assay dependent concentration.
Functional Studies-GYKI 52466(ab120336)
ab96379 staining MEK1 (phospho S298) in SK-N-SH cells treated with GYKI 52466 (ab120336), by ICC/IF. Decrease in MEK1 (phospho S298) expression correlates with increased concentration of GYKI 52466, as described in literature. The cells were incubated at 37°C for 1h in media containing different concentrations of ab120336 (GYKI 52466) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab96379 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody.
This product has been referenced in:
Szabados T et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res Bull55:387-91 (2001).
Read more (PubMed: 11489346) »
Johansen TH et al. Interactions among GYKI-52466, cyclothiazide, and aniracetam at recombinant AMPA and kainate receptors. Mol Pharmacol48:946-55 (1995).
Read more (PubMed: 7476926) »
Donevan SD & Rogawski MA GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron10:51-9 (1993).
Read more (PubMed: 7678966) »