PNU-282987 is a potent, selective α7 nAChR agonist with Ki of 26 nM, shows negligible block of α1β1γδ and α3β4 nAChRs (IC50>60 uM).
PNU-282987 is inactive at all tested monoamine, muscarine, glutamate, and GABA receptors.
PNU-282987 evokes whole-cell currents from cultured rat hippocampal neurons, improves the inherent hippocampal gating deficit occurring in a subpopulation of anesthetized rats, and enhances amphetamine-induced hippocampal oscillation; enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats.
