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14-September-2008 18:02:44 - Opioid receptor Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin/orphanin FQ. The opioid receptors are ~40% identical to somatostatin receptors SSTRs. Contents 1 Types of receptors 2 References 3 See also 4 External links Types of receptors There are three major subtypes of opioid receptors:1 Receptor Subtypes Location2 Function 2 delta δ OP1 I δ1, δ2 Brain pontine nuclei amygdala olfactory bulbs deep cortex analgesia antidepressant effects physical dependence kappa κ OP2 I κ1, κ2, κ3 Brain hypothalamus periaqueductal gray claustrum spinal cord substantia gelatinosa Spinal analgesia sedation miosis inhibition of ADH release mu μ OP3 I μ1, μ2, μ3 brain cortex laminae III and IV thalamus periaqueductal gray spinal cord substantia gelatinosa μ1: Supraspinal analgesia physical dependence μ2: respiratory depression miosis euphoria reduced GI motility physical dependence I. Name based on order of discovery Sigma receptors σ were once considered to be opioid receptors, but are not usually currently classified as such. The receptors were named using the first letter of the first ligand that was found to bind to them. Morphine was the first chemical shown to bind to mu receptors. The first letter of the drug morphine is `m', but in biochemistry there is a tendency to use Greek letters, thus turning the 'm' to μ. Similarly a drug known as ketocyclazocine was first shown to attach itself to kappa receptors.3 The opioid receptor types are ~70% identical with differences located at N and C termini. The μ receptor the μ represents morphine is perhaps the most important. It is thought that the G protein binds to the third intracellular loop of the opioid receptors. Both in mice and humans the genes for the various receptor subtypes are located on different chromosomes. Separate subtypes have been identified in human tissue. Research has so far failed to identify the genetic evidence of the subtypes, and it is thought that they arise from post-translational modification of cloned receptor types.4 An additional opioid receptor has been identified and cloned based on homology with the cDNA. This receptor is known as the nociceptin receptor or ORL 1 receptor. An IUPHAR International Union of Pharmacology subcommittee 200056 has recommended that appropriate terminology for the 3 classical μ, δ, κ receptors, and the non-classical nociceptin receptor, should be MOP, DOP, KOP and NOP respectively. References ^ Corbett AD, Henderson G, McKnight AT, Paterson SJ 2006. 75 years of opioid research: the exciting but vain quest for the Holy Grail. Br. J. Pharmacol. 147 Suppl 1: S153-62. doi:10.1038/sj.bjp.0706435. PMID 16402099. ^ a b Fine, Perry G.; Russell K. Portenoy 2004. Chapter 2: The Endogenous Opioid System, A Clinical Guide to Opioid Analgesia. McGraw Hill. ^ Anil Aggrawal 1995-05-01. Opium: the king of narcotics. BLTC Research. Retrieved on 2008-03-21. ^ Lemke, Thomas L.; Williams, David H.; Foye, William O. 2002. Opioid Analgesics; Fries, DS, Foye's principles of medicinal chemistry. Hagerstown, MD: Lippincott Williams Wilkins. ISBN 0-683-30737-1. ^ Cox BM, Chavkin C, Christie MJ, Civelli O, Evans C, Hamon MD, et al 2006. 75 years of opioid research: the exciting but vain quest for the Holy Grail. Br. J. Pharmacol. 147 Suppl 1: S153-62. doi:10.1038/sj.bjp.0706435. PMID 16402099. ^ Girdlestone, D October 2000. Opioid receptors; Cox BM, Chavkin C, Christie MJ, Civelli O, Evans C, Hamon MD, et al, The IUPHAR Compendium of Receptor Characterization and Classification, 2nd ion, London: IUPHAR Media, pages 321-333. See also Opioid antagonist External links MeSH Opioid+Receptors IUPHAR GPCR Database - Opioid Receptors. International Union of Basic and Clinical Pharmacology 2007-10-15. Retrieved on 2008-03-21. Corbett A, McKnight S, Henderson G. Opioid Receptors. BLTC Research. Retrieved on 2008-03-21. Lomize A, Lomize M, Pogozheva I. Orientations of Proteins in Membranes OPM database. University of Michigan. Retrieved on 2008-03-21. Mu-opioid receptor model inactive state with antagonist. Retrieved on 2008-03-21. Mu-opioid receptor model in active state with agonist. Retrieved on 2008-03-21. v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan GPR 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened v d e Neuropeptide receptors Hypothalamic hormone receptors CRH - FSH - LHRH - TRH - Somatostatin Pituitary hormone receptors Vasopressin 1A, 1B, 2 - Oxytocin - LHCG - Type I cytokine receptor GH, Prolactin - TSH Other hormone receptors Atrial natriuretic factor - Calcitonin - Cholecystokinin A, B - VIP Opioid receptors Delta - Kappa - Mu - Sigma 1, 2 - Nociceptin Other neuropeptide receptors Angiotensin - Bradykinin B1, B2 / Tachykinin TACR1 - Calcitonin gene-related peptide - Galanin - GPCR neuropeptide B/W, FF, S, Y - Neurotensin Retrieved from http://en..org/wiki/Opioid_receptor Categories: Cell signaling | Signal transduction | Opioid receptor Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Français Polski Suomi This page was last modified on 7 August 2008, at 14
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