Pitolisant HCl (formerly also known as BF2.649; BF2649; Ciproxidine; Wakix) is a nonimidazole-based inverse agonist of the recombinant human histamine H3 receptor approved in 2019 for the treatment of excessive daytime sleepiness in adults with narcolepsy.

PF-03654746 is a novel, potent, specific and selective histamine H3 receptor antagonist with >1000-fold selectivity for the H 3 receptor over the other histamine receptor subtypes. It is undergoing clinical trials for the treatment of ADHD, Tourette syndrome as well as potential anti-allergy applications. A previous clinical trial employing a nasal ragweed bolus after administration […]

Betahistine (also known as PT-9) is a potent histamine H3 receptor inhibitor with IC50 of 1.9 μM.

Pitolisant oxalate (formerly BF2649; BF2.649; Ciproxidine; Tiprolisant; Wakix), the oxalate salt of pitolisant, is a novel nonimidazole analog and an inverse agonist of the recombinant human histamine H3 receptor with Ki of 0.16 nM.