An inverse agonist of the histamine H ( 3 ) receptor improves wakefulness in narcolepsy : studies in orexin-/-mice and patients

@inproceedings{Lin2018AnIA,
  title={An inverse agonist of the histamine H ( 3 ) receptor improves wakefulness in narcolepsy : studies in orexin-/-mice and patients},
  author={Jian Sheng Lin and Yves Dauvilliers and Isabelle Arnulf and H{\'e}l{\`e}ne Bastuji and Christelle Anaclet and R{\'e}gis Parmentier and Laurence Kocher and M. Yanagisawa and Jian-Sheng Lin and Philippe Lehert and Xavier Ligneau and D. Perrin and Philippe Robert and Michel Roux and J. Lecomte and C. Schwartz},
  year={2018}
}
Narcolepsy is characterized by excessive daytime sleepiness(EDS), cataplexy, direct onsets of rapid eye movement(REM) sleep from wakefulness(DREMs) and deficiency of orexins, neuropeptides that promote wakefulness largely via activation of histamine(HA) pathways. The hypothesis that the orexin defect can be circumvented by enhancing HA release was explored in narcoleptic mice and patients using tiprolisant, an inverse H3-receptor agonist. In narcoleptic orexin-/-mice, tiprolisant enhanced HA… CONTINUE READING

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