GYKI-53655 1.25-7.5 mg/kg free base; was dissolved in 100% DMSO, and then diluted to a concentration of 2.5% DMSO, using a solution of 10% (w/v) (2-hydroxypropyl)-p-cyclodextrin in 5% (w/v) D-(+)-glucose monohydrate heated to 35-40 °C. Drug was administered to mice intraperitoneally (i.p.) 30 min prior to testing in an injection volume of 10 mL/kg.

Whole-cell voltage clamp recordings were made from single cells with use of the tight seal whole cell configuration of the patch-clamp technique. Glass fragments of coverslips with adherent cells (HEK293, expressing GluR1) were placed in a perfusion chamber and rinsed with buffer of composition 138 mM NaCl, 5 mM CaCl2, 5 mM KC1, 1 mM MgCl2, 10 mM HEPES and 10 mM glucose, pH to 7.5 with NaOH (osmolality 315 mosm/ kg). Pipette solutions contained 140 mM CsCl, 1 mM MgCl2, 14 mM diTris creatine phosphate, 50 U/ml creatine phosphokinase, 14 mM MgATP, 10 mM HEPES and 15 mM BAPTA, pH to 7.2 with CsOH (osmolality 295 mosm/kg). Experiments were performed at room temperature (20-22°C) and recorded on either a List EPC-7 or an Axopatch ID amplifier. Pipette resistances were typically 1.5-2.5 MQ. Drug application was via a series of perfusion lines to a multi-barrelled applicator (Biologic Inc.) and exchange of solutions under the present recording conditions was approximately 100 msec. LY-300168 inhibited AMPA (10uM)-mediated responses in recombinant human GluR1 receptors expressed in HEK293 cells with approximate IC50 of 5.9 uM.