Pitolisant shows high selectivity for H3 receptors compared with the other histamine receptor subtypes (H1, H2, and H4 subtypes) and shows a lack of interaction with other human receptors or channels.
In vivo
In animal experiments, pitolisant increases histaminergic and noradrenergic neuron activity, increases wakefulness at the expense of slow wave and rapid eye movement sleep, has low abuse potential, and has no effect on mechanical or thermal pain thresholds.