Orexin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

  • Paul Coleman Merck Research Laboratories
  • Luis de Lecea Scripps Research Institute
  • Anthony Gotter Merck Research Laboratories
  • Jim Hagan GlaxoSmithKline
  • Rebecca Hills University of Edinburgh
  • Thomas Kilduff SRI International
  • Jyrki P. Kukkonen University of Helsinki https://orcid.org/0000-0002-6989-1564
  • Rod Porter GlaxoSmithKline
  • John Renger Merck Research Laboratories
  • Jerome M Siegel University of California Los Angeles
  • Gregor Sutcliffe Scripps Research Institute
  • Neil Upton GlaxoSmithKline
  • Christopher J. Winrow Merck Research Laboratories


Orexin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Orexin receptors [39]) are activated by the endogenous polypeptides orexin-A and orexin-B (also known as hypocretin-1 and -2; 33 and 28 aa) derived from a common precursor, preproorexin or orexin precursor, by proteolytic cleavage and some typical peptide modifications [102]. Currently the only orexin receptor ligand in clinical use is suvorexant, which is used as a hypnotic. Orexin receptor crystal structures have been solved [124, 123].
How to Cite
Coleman, P., de Lecea, L., Gotter, A., Hagan, J., Hills, R., Kilduff, T., Kukkonen, J. P., Porter, R., Renger, J., Siegel, J. M., Sutcliffe, G., Upton, N. and Winrow, C. J. (2019) “Orexin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database”, IUPHAR/BPS Guide to Pharmacology CITE, 2019(4). doi: 10.2218/gtopdb/F51/2019.4.