阿片受体在GtoPdb v.2023.1

Anna Borsodi, Michael Bruchas, Girolamo Caló, Charles Chavkin, MacDonald J. Christie, Olivier Civelli, Mark Connor, Brian M. Cox, Lakshmi A. Devi, Christopher Evans, Volker Höllt, Graeme Henderson, Stephen Husbands, Eamonn Kelly, Brigitte Kieffer, Ian Kitchen, Mary-Jeanne Kreek, Lee-Yuan Liu-Chen, Davide Malfacini, Dominique Massot, Jean-Claude Meunier, Philip S. Portoghese, Stefan Schulz, Toni S. Shippenberg, Eric J. Simon, Lawrence Toll, John R. Traynor, Hiroshi Ueda, Yung H. Wong, Nurulain Zaveri, Andreas Zimmer
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引用次数: 1

摘要

阿片和阿片样受体可被多种内源性肽激活,包括[Met]脑啡肽(Met)、[Leu]脑啡肽(Leu)、β-内啡肽(β-end)、α-新啡肽、啡肽a (dynA)、啡肽B (dynB)、大啡肽(big dyn)、痛觉啡肽/啡肽FQ (N/OFQ);内啡肽-1和内啡肽-2也是潜在的内源性肽。阿片受体的希腊字母命名法为μ、δ和κ,这是公认的,NC-IUPHAR认为这种命名法是合适的,还有其拼写的符号(mu、delta和kappa),以及首字母缩略词MOP、DOP和KOP[122,101,92]。然而,缩略语MOR, DOR和KOR在文献中仍被广泛使用。人类N/OFQ受体NOP被认为是“阿片相关的”,而不是阿片样物质,因为它与传统的阿片样物质受体具有高度的结构同源性[304],但它具有不同的药理学。目前临床上使用的药物有很多,如吗啡和许多其他阿片类镇痛药,以及纳洛酮等拮抗剂。大多数临床使用的阿片类药物是相对选择性的μ激动剂或部分激动剂,尽管有一些μ/κ化合物,如布托啡诺在临床使用。κ阿片受体激动剂,如生物碱纳氟萘芬和外周作用肽difelikefalin,在临床用于治疗瘙痒。
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Opioid receptors in GtoPdb v.2023.1
Opioid and opioid-like receptors are activated by a variety of endogenous peptides including [Met]enkephalin (met), [Leu]enkephalin (leu), β-endorphin (β-end), α-neodynorphin, dynorphin A (dynA), dynorphin B (dynB), big dynorphin (Big dyn), nociceptin/orphanin FQ (N/OFQ); endomorphin-1 and endomorphin-2 are also potential endogenous peptides. The Greek letter nomenclature for the opioid receptors, μ, δ and κ, is well established, and NC-IUPHAR considers this nomenclature appropriate, along with the symbols spelled out (mu, delta, and kappa), and the acronyms, MOP, DOP, and KOP [124, 101, 92]. However the acronyms MOR, DOR and KOR are still widely used in the literature. The human N/OFQ receptor, NOP, is considered 'opioid-related' rather than opioid because, while it exhibits a high degree of structural homology with the conventional opioid receptors [304], it displays a distinct pharmacology. Currently there are numerous clinically used drugs, such as morphine and many other opioid analgesics, as well as antagonists such as naloxone. The majority of clinically used opiates are relatively selective μ agonists or partial agonists, though there are some μ/κ compounds, such as butorphanol, in clinical use. κ opioid agonists, such as the alkaloid nalfurafine and the peripherally acting peptide difelikefalin, are in clinical use for itch.
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