orexin receptor antagonists


Summary: Substances that bind to and inhibit the action of OREXIN RECEPTORS. Drugs in this class have been used as SLEEP AIDS.

Top Publications

  1. Rosini J, Dogra P. Pharmacology for insomnia: consider the options. Nursing. 2015;45:38-45; quiz 45-6 pubmed publisher
  2. Wilt T, MacDonald R, Brasure M, Olson C, Carlyle M, Fuchs E, et al. Pharmacologic Treatment of Insomnia Disorder: An Evidence Report for a Clinical Practice Guideline by the American College of Physicians. Ann Intern Med. 2016;165:103-12 pubmed publisher
    ..studies that reported harm information; FDA review data for nonbenzodiazepine hypnotics and orexin receptor antagonists; and product labels for all agents...
  3. Khoo S, McNally G, Clemens K. The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS ONE. 2017;12:e0173967 pubmed publisher
    ..Due to the increasing clinical use of dual orexin receptor antagonists in the treatment of disorders such as insomnia, we examined whether a dual orexin receptor antagonist ..
  4. Yao L, Ramirez A, Roecker A, Fox S, Uslaner J, Smith S, et al. The dual orexin receptor antagonist, DORA-22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine. J Neurochem. 2017;142:204-214 pubmed publisher
    ..Dual orexin receptor antagonists (DORAs) have recently emerged as an alternative therapeutic approach that acts via a distinct and more ..
  5. Beuckmann C, Suzuki M, Ueno T, Nagaoka K, Arai T, Higashiyama H. In Vitro and In Silico Characterization of Lemborexant (E2006), a Novel Dual Orexin Receptor Antagonist. J Pharmacol Exp Ther. 2017;362:287-295 pubmed publisher
    ..In silico modeling of lemborexant into the orexin receptors showed that it assumes the same type of conformation within the receptor-binding pocket as suvorexant, the ?-stacked horseshoe-like conformation. ..
  6. Boss C, Roch C. Orexin research: patent news from 2016. Expert Opin Ther Pat. 2017;27:1123-1133 pubmed publisher
    ..In addition, its activation via the Ox1 receptor triggers apoptosis in several cancer cell lines. Dual orexin receptor antagonists are successfully used to treat primary insomnia...
  7. Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, et al. The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468. J Pharmacol Exp Ther. 2017;362:489-503 pubmed publisher
    ..PBPK-PD modeling applied early in drug discovery, therefore, has great potential to assist in the identification of drug molecules when specific pharmacokinetic and pharmacodynamic requirements need to be met. ..
  8. Qiao S, Zhou W, Liu L, Zhang D, Zhong Y. Orexin-A Suppresses Signal Transmission to Dopaminergic Amacrine Cells From Outer and Inner Retinal Photoreceptors. Invest Ophthalmol Vis Sci. 2017;58:4712-4721 pubmed publisher
    ..Our results suggest that orexins could influence visual function via the dopaminergic system in the mammalian retina. ..
  9. Yamamoto N, Ohrui S, Okada T, Yata M, Saitoh T, Kutsumura N, et al. Essential structure of orexin 1 receptor antagonist YNT-707, Part I: Role of the 4,5-epoxy ring for binding with orexin 1 receptor. Bioorg Med Chem Lett. 2017;27:4176-4179 pubmed publisher