The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

Oprl1  -  opiate receptor-like 1

Rattus norvegicus

Synonyms: KOR-3, KOR3, Kappa-type 3 opioid receptor, LC132, MOR-C, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Oprl1


Psychiatry related information on Oprl1

  • An endogenous ligand of opioid receptor like 1, nociceptin is reported to inhibit light-induced phase shifts in locomotor activity rhythm [6].
  • 4. The anti-opioid effect of OFQ in rat brain and the high level of expression of LC132/ORL, receptor in the locus coeruleus indicated a possible role of OFQ in the precipitation of opiate withdrawal symptoms [7].
  • Pharmacological characterization of the nociceptin receptor which mediates reduction of alcohol drinking in rats [8].
  • These findings provide further evidence that selective agonists at the ORL-1 receptor attenuate ethanol intake in alcohol-preferring rats and suggest that the NC/ORL1 system may represent an interesting target for treatment of alcohol abuse [8].
  • Intracerebroventricular (i.c.v.) injection of OFQ (1 microgram) elicited a significant decrement of pain threshold which was abolished by the repeated pretreatment with antisense oligonucleotide (ASO) to OFQ receptor [9].

High impact information on Oprl1


Chemical compound and disease context of Oprl1

  • RATIONALE: Orphanin FQ (OFQ; also known as nociceptin), the endogenous ligand of the opioid receptor-like receptor, injected intracerebroventricularly (i.c.v.) decreases basal motor activity and basal extracellular levels of dopamine (DA) in the nucleus accumbens (Nuc Acc) in rats [15].
  • Estrogen was shown to increase ORL-1 immunoreactivity in the VMH, and microinfusions of OFQ/N into the VMH facilitated lordosis behavior in a dose-dependent manner [16].
  • In conclusion, N/OFQ receptor antagonist JTC-801 exerted anti-allodynic and anti-hyperalgesic effects in rats, suggesting that N/OFQ system might be involved in the modulation of neuropathic pain and inflammatory hyperalgesia [17].

Biological context of Oprl1

  • The amino acid sequence of ORL1 also shares a high degree of homology with that of mu receptor [18].
  • Nociceptin reversibly inhibited the DRP in a concentration-dependent manner (IC50: approximately 45 nM, maximal inhibition: approximately 50%), an effect that was antagonized by the ORL-1 receptor antagonist, J-113397 [2].
  • Two C-terminal amino acids, Ser(334) and Ser(335), are required for homologous desensitization and agonist-induced phosphorylation of opioid receptor-like 1 receptors [19].
  • The OFQR gene exceeds 10 kb in length and contains six exons ranging from 34 to 524 bp that are interrupted by five introns [20].
  • These data suggest that unique regions in intron 1 and in the 5' flanking region of the OFQR gene contribute to the regulation of its expression in different tissues [20].

Anatomical context of Oprl1


Associations of Oprl1 with chemical compounds

  • An opioid receptor like 1 antagonist, compound B (10 microM), induced a phase delay, and this effect was blocked by nociceptin (10 microM) [6].
  • Substituting Ser(334) or Ser(335) with alanine greatly impaired nociceptin-induced ORL1 desensitization [19].
  • In HEK 293 cells expressing wild-type ORL1 and ORL1(CDelta21), which lacks C-terminal 21 amino acids, nociceptin inhibition of adenylate cyclase activity exhibited homologous desensitization after 1 h pretreatment of nociceptin [19].
  • In the present study, we investigated the functional role played by C-terminal Ser/Thr residues in agonist-induced desensitization and phosphorylation of ORL1 [19].
  • The cellular localization of ORL-1 receptors and activated G-proteins in area 24 was examined using two strategies: ibotenic acid injection into the cortex or undercut lesions to remove afferent axons, followed by autoradiography [24].

Regulatory relationships of Oprl1


Other interactions of Oprl1

  • 1. Whole-cell patch clamp recordings were made from rat rostral ventromedial medulla (RVM) neurons in vitro to investigate the cellular actions of the opioid-like receptor ORL1 (NOP), ligand nociceptin/orphanin FQ and other putative prepronociceptin products [25].
  • These observations indicate that MOR and ORL-1 receptors are expressed predominantly on different fiber systems in these regions [21].
  • These converging antagonist and AS ODN data firmly implicate the kappa(1)-opioid receptor and the KOR-1 and KOR-3/ORL-1 opioid receptor genes in the mediation of dynorphin-induced feeding [26].
  • Nociceptin, an endogenous ligand for the opioid receptor-like (ORL-1) G-protein coupled receptor, has been found to inhibit the local axon reflex-mediated neurogenic inflammation by suppressing the release of vasoactive neuropeptides from sensory afferent terminals [2].
  • The DRG cell line F11 was found to express preproN/OFQ, but not ORL1, and, therefore, is well suited to study the mechanisms of N/OFQ gene regulation in vitro [3].

Analytical, diagnostic and therapeutic context of Oprl1


  1. Antisense mapping of opioid receptor clones: effects upon 2-deoxy-D-glucose-induced hyperphagia. Burdick, K., Yu, W.Z., Ragnauth, A., Moroz, M., Pan, Y.X., Rossi, G.C., Pasternak, G.W., Bodnar, R.J. Brain Res. (1998) [Pubmed]
  2. Activation of spinal ORL-1 receptors prevents acute cutaneous neurogenic inflammation: role of nociceptin-induced suppression of primary afferent depolarization. Dong, X.W., Williams, P.A., Jia, Y.P., Priestley, T. Pain (2002) [Pubmed]
  3. Relationship of pronociceptin/orphanin FQ and the nociceptin receptor ORL1 with substance P and calcitonin gene-related peptide expression in dorsal root ganglion of the rat. Mika, J., Li, Y., Weihe, E., Schafer, M.K. Neurosci. Lett. (2003) [Pubmed]
  4. Opioid receptor-like 1 stimulation in the collecting duct induces aquaresis through vasopressin-independent aquaporin-2 downregulation. Hadrup, N., Petersen, J.S., Praetorius, J., Meier, E., Graebe, M., Brønd, L., Staahltoft, D., Nielsen, S., Christensen, S., Kapusta, D.R., Jonassen, T.E. Am. J. Physiol. Renal Physiol. (2004) [Pubmed]
  5. Nociceptin and the ORL-1 ligand [Phe1psi (CH2-NH)Gly2]nociceptin(1-13)NH2 exert anti-opioid effects in the Freund's adjuvant-induced arthritic rat model of chronic pain. Bertorelli, R., Corradini, L., Rafiq, K., Tupper, J., Calò, G., Ongini, E. Br. J. Pharmacol. (1999) [Pubmed]
  6. Role of nociceptin and opioid receptor like 1 on entrainment function in the rat suprachiasmatic nucleus. Sugino, T., Shimazoe, T., Ikeda, M., Watanabe, S. Neuroscience (2006) [Pubmed]
  7. Bidirectional modulatory effect of orphanin FQ on morphine-induced analgesia: antagonism in brain and potentiation in spinal cord of the rat. Tian, J.H., Xu, W., Fang, Y., Mogil, J.S., Grisel, J.E., Grandy, D.K., Han, J.S. Br. J. Pharmacol. (1997) [Pubmed]
  8. Pharmacological characterization of the nociceptin receptor which mediates reduction of alcohol drinking in rats. Ciccocioppo, R., Polidori, C., Antonelli, L., Salvadori, S., Guerrini, R., Massi, M. Peptides (2002) [Pubmed]
  9. Antagonistic action of orphanin FQ on acupuncture analgesia in rat brain. Zhu, C.B., Xu, S.F., Cao, X.D., Wu, G.C., Zhang, X.L., Li, M.Y., Cui, D.F., Chi, C.W. Acupuncture & electro-therapeutics research. (1996) [Pubmed]
  10. Orphanin FQ causes contractions via inhibiting purinergic pathway in the rat colon. Takahashi, T., Bagnol, D., Schneider, D., Mizuta, Y., Ishiguchi, T., LePard, K., Galligan, J.J., Watson, S.J., Owyang, C. Gastroenterology (2000) [Pubmed]
  11. Chronic heroin self-administration desensitizes mu opioid receptor-activated G-proteins in specific regions of rat brain. Sim-Selley, L.J., Selley, D.E., Vogt, L.J., Childers, S.R., Martin, T.J. J. Neurosci. (2000) [Pubmed]
  12. Actions of the ORL1 receptor ligand nociceptin on membrane properties of rat periaqueductal gray neurons in vitro. Vaughan, C.W., Ingram, S.L., Christie, M.J. J. Neurosci. (1997) [Pubmed]
  13. Moving from the orphanin FQ receptor to an opioid receptor using four point mutations. Meng, F., Taylor, L.P., Hoversten, M.T., Ueda, Y., Ardati, A., Reinscheid, R.K., Monsma, F.J., Watson, S.J., Civelli, O., Akil, H. J. Biol. Chem. (1996) [Pubmed]
  14. Creating a functional opioid alkaloid binding site in the orphanin FQ receptor through site-directed mutagenesis. Meng, F., Ueda, Y., Hoversten, M.T., Taylor, L.P., Reinscheid, R.K., Monsma, F.J., Watson, S.J., Civelli, O., Akil, H. Mol. Pharmacol. (1998) [Pubmed]
  15. Orphanin FQ/nociceptin attenuates motor stimulation and changes in nucleus accumbens extracellular dopamine induced by cocaine in rats. Lutfy, K., Do, T., Maidment, N.T. Psychopharmacology (Berl.) (2001) [Pubmed]
  16. Orphanin FQ/nociceptin in the ventromedial nucleus facilitates lordosis in female rats. Sinchak, K., Hendricks, D.G., Baroudi, R., Micevych, P.E. Neuroreport (1997) [Pubmed]
  17. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Tamai, H., Sawamura, S., Takeda, K., Orii, R., Hanaoka, K. Eur. J. Pharmacol. (2005) [Pubmed]
  18. Heterodimerization of opioid receptor-like 1 and mu-opioid receptors impairs the potency of micro receptor agonist. Wang, H.L., Hsu, C.Y., Huang, P.C., Kuo, Y.L., Li, A.H., Yeh, T.H., Tso, A.S., Chen, Y.L. J. Neurochem. (2005) [Pubmed]
  19. Two C-terminal amino acids, Ser(334) and Ser(335), are required for homologous desensitization and agonist-induced phosphorylation of opioid receptor-like 1 receptors. Wang, H.L., Kuo, Y.L., Hsu, C.Y., Huang, P.C., Li, A.H., Chou, A.H., Yeh, T.H., Chen, Y.L. Cell. Signal. (2006) [Pubmed]
  20. Molecular cloning of the orphanin FQ receptor gene and differential tissue expression of splice variants in rat. Currò, D., Yoo, J.H., Anderson, M., Song, I., Del Valle, J., Owyang, C. Gene (2001) [Pubmed]
  21. ORL-1 and mu opioid receptor antisera label different fibers in areas involved in pain processing. Monteillet-Agius, G., Fein, J., Anton, B., Evans, C.J. J. Comp. Neurol. (1998) [Pubmed]
  22. Opioid receptor-like 1 (NOP) receptors in the rat dorsal raphe nucleus: evidence for localization on serotoninergic neurons and functional adaptation after 5,7-dihydroxytryptamine lesion. Le Maître, E., Vilpoux, C., Costentin, J., Leroux-Nicollet, I. J. Neurosci. Res. (2005) [Pubmed]
  23. cDNA cloning and regional distribution of a novel member of the opioid receptor family. Fukuda, K., Kato, S., Mori, K., Nishi, M., Takeshima, H., Iwabe, N., Miyata, T., Houtani, T., Sugimoto, T. FEBS Lett. (1994) [Pubmed]
  24. Distribution of ORL-1 receptor binding and receptor-activated G-proteins in rat forebrain and their experimental localization in anterior cingulate cortex. Sim-Selley, L.J., Vogt, L.J., Childers, S.R., Vogt, B.A. Neuropharmacology (2003) [Pubmed]
  25. Actions of nociceptin/orphanin FQ and other prepronociceptin products on rat rostral ventromedial medulla neurons in vitro. Vaughan, C.W., Connor, M., Jennings, E.A., Marinelli, S., Allen, R.G., Christie, M.J. J. Physiol. (Lond.) (2001) [Pubmed]
  26. Dynorphin A(1-17)-induced feeding: pharmacological characterization using selective opioid antagonists and antisense probes in rats. Silva, R.M., Grossman, H.C., Hadjimarkou, M.M., Rossi, G.C., Pasternak, G.W., Bodnar, R.J. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
WikiGenes - Universities