orexin receptors


Summary: G-protein-coupled NEUROPEPTIDE RECEPTORS that have specificity for OREXINS and play a role in appetite control, and sleep-wake cycles. Two principle receptor types exist, each having a specificity for OREXIN A and OREXIN B peptide subtypes.

Top Publications

  1. Rosini J, Dogra P. Pharmacology for insomnia: consider the options. Nursing. 2015;45:38-45; quiz 45-6 pubmed publisher
  2. 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
    ..Lemborexant binds to both orexin receptors and functionally inhibits them in a competitive manner with low nanomolar potency, without any species ..
  3. Boss C, Roch C. Orexin research: patent news from 2016. Expert Opin Ther Pat. 2017;27:1123-1133 pubmed publisher
    ..Expert opinion: The large number of patents shows the continuing interest in the orexin receptors as targets. The structural scope covered is narrow. Questions about novelty and inventiveness are evident...
  4. Joshi D, Sarkar D, Singh S. Decreased expression of orexin 1 receptor in adult mice testes during alloxan-induced diabetes mellitus perturbs testicular steroidogenesis and glucose homeostasis. Biochem Biophys Res Commun. 2017;490:1346-1354 pubmed publisher
  5. 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
  6. Futamura A, Nozawa D, Araki Y, Tamura Y, Tokura S, Kawamoto H, et al. Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide. Bioorg Med Chem. 2017;25:5203-5215 pubmed publisher
    ..01nM and a 265-fold selectivity for orexin receptor 1 over orexin receptor 2. ..
  7. Wan X, Liu Y, Zhao Y, Sun X, Fan D, Guo L. Orexin A affects HepG2 human hepatocellular carcinoma cells glucose metabolism via HIF-1?-dependent and -independent mechanism. PLoS ONE. 2017;12:e0184213 pubmed publisher
    ..These findings provide new insight into the regulation of glucose metabolism by orexin A in hepatocellular carcinoma cells. ..
  8. Turku A, Rinne M, Boije af Gennäs G, Xhaard H, Lindholm D, Kukkonen J. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS ONE. 2017;12:e0178526 pubmed publisher
    ..However, a major fraction of the response was not mediated by orexin receptors, as determined utilizing the non-selective orexin receptor antagonist N-biphenyl-2-yl-1-{[(1-methyl-1H-..
  9. Modi H, Wang Q, Gd S, Sherman D, Greenwald E, Savonenko A, et al. Intranasal post-cardiac arrest treatment with orexin-A facilitates arousal from coma and ameliorates neuroinflammation. PLoS ONE. 2017;12:e0182707 pubmed publisher
    ..At 4hrs post-CA, the mRNA levels of proinflammatory markers (IL1?, iNOS, TNF-?, GFAP, CD11b) and orexin receptors (ORX1R and ORX2R) were examined in different brain regions...