Pitolisant

Из Википедије, слободне енциклопедије

{{chembox-lat | Verifiedfields = | verifiedrevid = 464208162 |ImageFile=BF2649_structure.png |ImageSize=200px |IUPACName=1-{3-[3-(4-hlorofenil)propoksi]propil}piperidin |OtherNames= BF2.649 |Section1=! colspan=2 style="background: #f8eaba; text-align: center;" |Identifikacija

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CAS broj

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3D model (Jmol)

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| ChemSpider

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PubChem[1][2] CID

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Hemijska formula

| C17H26ClNO

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| 295,846 g/mol

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Pitolisant (INN) ili tiprolisant (USAN) je inverzni agonist/antagonist histaminskog receptora koji je selektivan za H3 receptor.[3] On ima stimulantne i nootropne efekte u životinjskim studijama,[4] i može da ima nekoliko potencijalnih medicinskih primena. Istražen je za tretman narkolepsije, i za tu indikaciju mu je odobren status orfan leka u EU i SAD.[5][6] On je u kliničkim ispitivanjima za šizofreniju i Parkinsonova bolest.[6][7][8]

Pitolisant je razvijen nakon otkrića H3 receptora.[9] Pitolisant je prvi inverzni agonist H3 receptora sa kliničkom primenom.

Reference[уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today. 15 (23-24): 1052—7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton; Yanli Wang; Paul A. Thiessen; Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry. 4: 217—241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Celanire S, Wijtmans M, Talaga P, Leurs R, de Esch IJ (2005). „Keynote review: histamine H3 receptor antagonists reach out for the clinic”. Drug Discov. Today. 10 (23-24): 1613—27. PMID 16376822. doi:10.1016/S1359-6446(05)03625-1. 
  4. -{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 [13-[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
  5. 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
  6. 6,0 6,1 Prous Science: Molecule of the Month September 2011
  7. 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
  8. Stocking EM, Letavic MA (2008). „Histamine H3 antagonists as wake-promoting and pro-cognitive agents”. Current Topics in Medicinal Chemistry. 8 (11): 988—1002. PMID 18673168. doi:10.2174/156802608784936728. 
  9. Schwartz, Jean-Charles. The histamine H3 receptor: from discovery to clincial trials with pitolisant. BPJ 2011 May [1]

Spoljašnje veze[уреди]