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|Section2= |Section3= }} Pitolisant (INN) or tiprolisant (USAN) is a histamine receptor inverse agonist/antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies,〔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 , 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〕 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.〔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〕〔 It is currently in clinical trials for schizophrenia and Parkinson's disease.〔(Prous Science: Molecule of the Month September 2011 )〕〔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〕 Pitolisant was developed by Jean-Charles Schwartz, Walter Schunack and colleagues after the former discovered H3 receptors. Pitolisant was the first clinically used H3 receptor inverse agonist. ==References== 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Pitolisant」の詳細全文を読む スポンサード リンク
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