Pitolisant

• CAT Number: I003332
• CAS Number: 362665-56-3
• Molecular Formula: C17H26ClNO
• Molecular Weight: 295.85
• Purity: ≥95%
• Target: Histamine Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.16 nM (Ki value); 1.5 nM (EC50) [1]

Pitolisant(CAT: I003332) is a novel and selective nonimidazole inverse agonist at the recombinant human H3 receptor. It acts as a histamine H3 receptor antagonist/inverse agonist, which modulates the release of various neurotransmitters in the brain. Pitolisant has been investigated for its use in the treatment of narcolepsy, a neurological disorder characterized by excessive daytime sleepiness and abnormal sleep-wake cycles. It has shown efficacy in improving wakefulness and reducing excessive daytime sleepiness in patients with narcolepsy. Pitolisant is also being explored for its potential in other sleep disorders and psychiatric conditions.

Reference

[1]. Ligneau X, Perrin D, Landais L, 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. 2007 Jan;320(1):365-75.
[2]. Kasteleijn-Nolst Trenité D, Parain D, Genton P, Efficacy of the histamine 3 receptor (H3R) antagonist pitolisant (formerly known as tiprolisant; BF2.649) in epilepsy: Dose-dependent effects in the human photosensitivity model. Epilepsy Behav. 2013 Jul;28(1):66-70.
[3]. Ligneau X, Landais L, Perrin D, Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649. Biochem Pharmacol. 2007 Apr 15;73(8):1215-24.