Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat

  title={Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat},
  author={Christine Dugovic and Jonathan E. Shelton and Leah Aluisio and Ian C. Fraser and Xiaohui Jiang and Steven W. Sutton and Pascal Bonaventure and Sujin Yun and Xiaorong Li and Brian Lord and Curt A. Dvorak and Nicholas I. Carruthers and Timothy W. Lovenberg},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={142 - 151}
Orexins are peptides produced by lateral hypothalamic neurons that exert a prominent role in the maintenance of wakefulness by activating orexin-1 (OX1R) and orexin-2 (OX2R) receptor located in wake-active structures. Pharmacological blockade of both receptors by the dual OX1/2R antagonist (2R)-2-[(1S)-6,7-dimethoxy-1-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydroisoquinolin-2(1H)-yl]-N-methyl-2-phenylethanamide (almorexant) has been shown to promote sleep in animals and humans during their… 

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Arousal effect of orexin A depends on activation of the histaminergic system

  • Zhi-Li HuangW. Qu O. Hayaishi
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 2001
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