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Tiprolisant
BF2649 structure.png
IUPAC name
Identifiers
CAS number 903576-44-3
SMILES
Properties
Molecular formula C17H26ClNO
Molar mass 295.85 g mol−1
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

Tiprolisant (BF2.649) 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[3] and is currently in clinical trials for schizophrenia.[4][5]

References

  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. http://linkinghub.elsevier.com/retrieve/pii/S1359-6446(05)03625-1.  
  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. ^ 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
  5. ^ 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.  
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