Nociceptin receptor

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Opiate receptor-like 1
Identifiers
SymbolsOPRL1; KOR-3; MGC34578; NOCIR; OOR; ORL1
External IDsOMIM: 602548 MGI: 97440 HomoloGene: 22609 IUPHAR: NOP GeneCards: OPRL1 Gene
Orthologs
SpeciesHumanMouse
Entrez498718389
EnsemblENSG00000125510ENSMUSG00000027584
UniProtP41146Q542U1
RefSeq (mRNA)XM_001131314NM_011012
RefSeq (protein)XP_001131314NP_035142
Location (UCSC)Chr 20:
62.71 - 62.74 Mb		Chr 2:
181.64 - 181.65 Mb
PubMed search[1][2]

The nociceptin receptor or NOP also known as the orphanin FQ receptor or kappa-type 3 opioid receptor is a protein that in humans is encoded by the OPRL1 (opiate receptor-like 1) gene.[1] The nociceptin receptor is a G protein-coupled receptor whose natural ligand is known as nociceptin or orphanin FQ, a 17 amino acid neuropeptide.[2] This receptor is involved in the regulation of numerous brain activities, particularly instinctive and emotional behaviors.[3]

Mechanism

Nociceptin is thought to be an endogenous antagonist of dopamine transport that may act either directly on dopamine or by inhibiting GABA to affect dopamine levels.[4] Within the central nervous system its action can be either similar or opposite to those of opioids depending on their location.[5] It controls a wide range of biological functions ranging from nociception to food intake, from memory processes to cardiovascular and renal functions, from spontaneous locomotor activity to gastrointestinal motility, from anxiety to the control of neurotransmitter release at peripheral and central sites.[5]

Selective ligands

Several commonly used opioid drugs including etorphine and buprenorphine have been demonstrated to bind to nociceptin receptors, but this binding is relatively insignificant compared to their activity at other opioid receptors. More recently a range of selective ligands for ORL-1 have been developed, which show little or no affinity to other opioid receptors and so allow ORL-1 mediated responses to be studied in isolation.

Agonists

  • Buprenorphine (not selective for ORL-1, also partial agonist of µ-opioid receptor and competitive antagonist of ϰ-opioid receptors)
  • Nociceptin
  • Norbuprenorphine (not selective for ORL-1, also full agonist at μ-opioid receptors)
  • NNC 63-0532
  • Ro64-6198
  • Ro65-6570
  • SCH-221,510
  • SR-16435 (mixed mu / nociceptin partial agonist)

Antagonists

Applications

ORL 1 agonists are being studied as treatments for heart failure and migraine[6] while nociceptin antagonists such as JTC-801 may have analgesic[7] and antidepressant qualities.[8]

The novel drug buprenorphine is a partial agonist at ORL 1 receptors while its metabolite norbuprenorphine is a full agonist at these receptors.[9]

References

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Further reading

  • Mollereau C, Mouledous L (2000). "Tissue distribution of the opioid receptor-like (ORL1) receptor". Peptides. 21 (7): 907–17. doi:10.1016/S0196-9781(00)00227-8. PMID 10998524. 
  • New DC, Wong YH (2003). "The ORL1 receptor: molecular pharmacology and signalling mechanisms". Neurosignals. 11 (4): 197–212. doi:10.1159/000065432. PMID 12393946. 
  • Zaveri N (2003). "Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents". Life Sci. 73 (6): 663–78. doi:10.1016/S0024-3205(03)00387-4. PMID 12801588. 
  • Wick MJ, Minnerath SR, Roy S; et al. (1996). "Expression of alternate forms of brain opioid 'orphan' receptor mRNA in activated human peripheral blood lymphocytes and lymphocytic cell lines". Brain Res. Mol. Brain Res. 32 (2): 342–7. doi:10.1016/0169-328X(95)00096-B. PMID 7500847. 
  • Meunier JC, Mollereau C, Toll L; et al. (1995). "Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor". Nature. 377 (6549): 532–5. doi:10.1038/377532a0. PMID 7566152. 
  • Yung LY, Joshi SA, Chan RY; et al. (1999). "GalphaL1 (Galpha14) couples the opioid receptor-like1 receptor to stimulation of phospholipase C". J. Pharmacol. Exp. Ther. 288 (1): 232–8. PMID 9862775. 
  • Feild JA, Foley JJ, Testa TT; et al. (1999). "Cloning and characterization of a rabbit ortholog of human Galpha16 and mouse G(alpha)15". FEBS Lett. 460 (1): 53–6. doi:10.1016/S0014-5793(99)01317-4. PMID 10571060. 
  • Mouledous L, Topham CM, Moisand C; et al. (2000). "Functional inactivation of the nociceptin receptor by alanine substitution of glutamine 286 at the C terminus of transmembrane segment VI: evidence from a site-directed mutagenesis study of the ORL1 receptor transmembrane-binding domain". Mol. Pharmacol. 57 (3): 495–502. PMID 10692489. 
  • Yung LY, Tsim KW, Pei G, Wong YH (2000). "Immunoglobulin G1 Fc fragment-tagged human opioid receptor-like receptor retains the ability to inhibit cAMP accumulation". Biological signals and receptors. 9 (5): 240–7. doi:10.1159/000014645. PMID 10965058. 
  • Ito E, Xie G, Maruyama K, Palmer PP (2000). "A core-promoter region functions bi-directionally for human opioid-receptor-like gene ORL1 and its 5'-adjacent gene GAIP". J. Mol. Biol. 304 (3): 259–70. doi:10.1006/jmbi.2000.4212. PMID 11090272. 
  • Okada K, Sujaku T, Chuman Y; et al. (2001). "Highly potent nociceptin analog containing the Arg-Lys triple repeat". Biochem. Biophys. Res. Commun. 278 (2): 493–8. doi:10.1006/bbrc.2000.3822. PMID 11097863. 
  • Serhan CN, Fierro IM, Chiang N, Pouliot M (2001). "Cutting edge: nociceptin stimulates neutrophil chemotaxis and recruitment: inhibition by aspirin-triggered-15-epi-lipoxin A4". J. Immunol. 166 (6): 3650–4. PMID 11238602. 
  • Deloukas P, Matthews LH, Ashurst J; et al. (2002). "The DNA sequence and comparative analysis of human chromosome 20". Nature. 414 (6866): 865–71. doi:10.1038/414865a. PMID 11780052. 
  • Mandyam CD, Thakker DR, Christensen JL, Standifer KM (2002). "Orphanin FQ/nociceptin-mediated desensitization of opioid receptor-like 1 receptor and mu opioid receptors involves protein kinase C: a molecular mechanism for heterologous cross-talk". J. Pharmacol. Exp. Ther. 302 (2): 502–9. doi:10.1124/jpet.102.033159. PMID 12130708. 
  • Thakker DR, Standifer KM (2003). "Orphanin FQ/nociceptin blocks chronic morphine-induced tyrosine hydroxylase upregulation". Brain Res. Mol. Brain Res. 105 (1-2): 38–46. doi:10.1016/S0169-328X(02)00390-X. PMID 12399106. 
  • Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932. 
  • Spampinato S, Di Toro R, Alessandri M, Murari G (2003). "Agonist-induced internalization and desensitization of the human nociceptin receptor expressed in CHO cells". Cell. Mol. Life Sci. 59 (12): 2172–83. doi:10.1007/s000180200016. PMID 12568343. 

External links

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(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) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
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, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
Hormone receptors
Other
Opioid receptors
Delta - Kappa - Mu - Sigma (1, 2) - Nociceptin
Other neuropeptide receptors
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  3. ↑ "Entrez Gene: OPRL1 opiate receptor-like 1". 
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