New nanomolar negative modulators of AMPA receptors

Bisamides of 1,4-bis(aminomethyl)benzene with cyclopropane-, cyclobutane- and cyclopentanecarboxylic acids reveal the negative modulation of kainate-induced currents in rat Purkinje neurons observed using patch clamp technique. The most pronounced effect has been found for the bisamide of cyclobutanecarboxylic acid, which blocks the currents by 41 and 49% at concentrations of 1×10⁻¹⁰ and 1×10⁻⁹moldm⁻³, respectively.