Non-competitive AMPA and kainate receptor antagonist. (IC50 values for inhibition of AMPA-mediated responses in cells expressing human GluR1 and GluR4 are 6 and 5 µM, respectively). Analog of GYKI 52466 (ab120336). Anticonvulsant in vivo. At higher concentrations blocks GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM).
Also available in simple stock solutions (ab144499) - add 1 ml of water to get an exact, ready-to-use concentration.
Store at +4°C. The product can be stored for up to 12 months.
Soluble in water to 100 mM and in DMSO to 100 mM
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.
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) »
Partin KM & Mayer ML Negative allosteric modulation of wild-type and mutant AMPA receptors by GYKI 53655. Mol Pharmacol49:142-8 (1996).
Read more (PubMed: 8569699) »
Bleakman D et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology35:1689-702 (1996).
Read more (PubMed: 9076748) »