Pitolisant

Pitolisant is a nonimidazole histamine H₃ receptor antagonist (K_i = 0.16 nM) and inverse agonist (EC₅₀ = 1.5 nM).¹ It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED₅₀ value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.² When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.

WARNING This product is not for human or veterinary use.

1. Ligneau, X., Perrin, D., Landais, L., et al. BF2.649 [1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J. Pharmacol. Exp. Ther. 320(1), 365-375 (2007).

2. Brabant, C., Charlier, Y., and Tirelli, E. The histamine H₃-receptor inverse agonist pitolisant improves fear memory in mice. Behav. Brain Res. 243, 199-204 (2013).