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Orexin receptors in GtoPdb v.2025.3

Title: Orexin receptors in GtoPdb v.2025.3
Authors: Aston-Jones, Gary; Winrow, Christopher J.; Upton, Neil; Sutcliffe, J. Gregor; Siegel, Jerome M; Sakurai, Takeshi; Renger, John; Porter, Rod; McDonald, Terrence P.; Kukkonen, Jyrki P.; Kilduff, Thomas; Jacobson, Laura H.; Hoyer, Daniel; Hartman, Debbie; de Lecea, Luis; Coleman, Paul; Bonaventure, Pascal; Yanagisawa, Masashi
Source: IUPHAR/BPS Guide to Pharmacology CITE; Vol. 2025 No. 3 (2025) ; 2633-1020
Publisher Information: University of Edinburgh
Publication Year: 2025
Description: Orexin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Orexin receptors [79]) 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, prepro-orexin or orexin precursor, by proteolytic cleavage and some typical peptide modifications [120, 79]. Orexin signaling has been associated with regulation of sleep and wakefulness, reward and addiction, appetite and feeding, pain gating, stress response, anxiety and depression. Currently the orexin receptor ligands in clinical use are the dual orexin receptor antagonists suvorexant, lemborexant and daridorexant, which are used as hypnotics, and several dual, as well as OX1- and OX2-selective antagonists are under development for different indications. Multiple orexin agonists are in development for the treatment of narcolepsy and other sleep disorders. Orexin receptor 3D structures have been solved [150, 148, 55, 130, 47, 113, 7, 149].
Document Type: article in journal/newspaper
File Description: application/pdf; text/html
Language: English
Relation: https://journals.ed.ac.uk/gtopdb-cite/article/view/11722/14119; https://journals.ed.ac.uk/gtopdb-cite/article/view/11722/14117; https://journals.ed.ac.uk/gtopdb-cite/article/view/11722/14118
DOI: 10.2218/gtopdb/F51/2025.3
Availability: https://journals.ed.ac.uk/gtopdb-cite/article/view/11722; https://doi.org/10.2218/gtopdb/F51/2025.3
Rights: Copyright (c) 2025 The authors ; http://creativecommons.org/licenses/by-sa/4.0
Accession Number: edsbas.51011297
Database: BASE