From Wikipedia, the free encyclopedia
Jump to: navigation, search
Pitolisant skeletal.svg
IUPAC name
Other names
903576-44-3 N
ChEMBL ChEMBL462605 YesY
ChemSpider 8123714 YesY
Jmol-3D images Image
PubChem 9948102
Molar mass 295.85 g·mol−1
Except where noted otherwise, data is given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
 N verify (what isYesY/N?)
Infobox references

Pitolisant (INN) or tiprolisant (USAN) is a histamine receptor inverse agonist/antagonist selective for the H3 subtype.[1] It has stimulant and nootropic effects in animal studies,[2] and may have several medical applications, having been researched for the treatment of narcolepsy, for which it has been granted orphan drug status in the EU and US.[3][4] It is currently in clinical trials for schizophrenia and Parkinson's disease.[4][5][6]

Pitolisant was developed by Jean-Charles Schwartz and colleagues after the former discovered H3 receptors.[7] Pitolisant was the first clinically used H3 receptor inverse agonist.


  1. ^ Celanire S, Wijtmans M, Talaga P, Leurs R, de Esch IJ (December 2005). "Keynote review: histamine H3 receptor antagonists reach out for the clinic". Drug Discov. Today 10 (23-24): 1613–27. doi:10.1016/S1359-6446(05)03625-1. PMID 16376822. 
  2. ^ Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, Berrebi-Bertrand I, Lecomte JM, Parmentier R, Anaclet C, Lin JS, Bertaina-Anglade V, la Rochelle CD, d'Aniello F, Rouleau A, Gbahou F, Arrang JM, Ganellin CR, Stark H, Schunack W, Schwartz JC. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. Journal of Pharmacology and Experimental Therapeutics. 2007 Jan;320(1):365-75. PMID 17005916
  3. ^ Lin JS, Dauvilliers Y, Arnulf I, Bastuji H, Anaclet C, Parmentier R, Kocher L, Yanagisawa M, Lehert P, Ligneau X, Perrin D, Robert P, Roux M, Lecomte JM, Schwartz JC. An inverse agonist of the histamine H(3) receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients. Neurobiology of Disease. 2008 Apr;30(1):74-83. PMID 18295497
  4. ^ a b Prous Science: Molecule of the Month September 2011
  5. ^ Ligneau X, Landais L, Perrin D, Piriou J, Uguen M, Denis E, Robert P, Parmentier R, Anaclet C, Lin JS, Burban A, Arrang JM, Schwartz JC. Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649. Biochemical Pharmacology. 2007 Apr 15;73(8):1215-24. PMID 17343831
  6. ^ Stocking EM, Letavic MA (2008). "Histamine H3 antagonists as wake-promoting and pro-cognitive agents". Current Topics in Medicinal Chemistry 8 (11): 988–1002. doi:10.2174/156802608784936728. PMID 18673168. 
  7. ^ Schwartz, Jean-Charles (May 2011). "The histamine H3 receptor: from discovery to clinical trials with pitolisant". BPJ. doi:10.1111/j.1476-5381.2011.01286.x.