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OPRD1  -  opioid receptor, delta 1

Sus scrofa

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Disease relevance of OPRD1


Psychiatry related information on OPRD1

  • These data show that (+)-21 and (+)-22 are potent delta receptor agonists and suggest that these compounds will be valuable tools for further study of the delta opioid receptor at the molecular level, including its function and role in analgesia and drug abuse [3].

High impact information on OPRD1

  • The delta-opioid receptor affinity labeled and purified to homogeneity from NG108-15 cells comprises a glycoprotein subunit of Mr58,000 with one mol ligand bound/mol protein [4].
  • In binding assays with membranes from guinea pig brain, ethylketocyclazocine and dynorphin-(1--13) amide were more potent in displacing tritium-labeled ethylketocyclazocine than in displacing typical mu and delta opioid receptor ligands [5].
  • To determine the cellular sites for DOR-mediated actions, we examined the ultrastructural localization of DOR and Met5-enkephalin (ME) in the spinal cord by combining immunoperoxidase and immunogold-silver labeling for antibodies against DOR and ME, respectively [1].
  • Ultrastructural immunolabeling shows prominent presynaptic vesicular localization of delta-opioid receptor within both enkephalin- and nonenkephalin-containing axon terminals in the superficial layers of the rat cervical spinal cord [1].
  • Overall, the data collected demonstrate that the putative prodermorphin product Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 named dermenkephalin, behaves as a potent delta opioid agonist exhibiting high affinity and high selectivity for the delta opioid receptor [6].

Biological context of OPRD1


Anatomical context of OPRD1

  • Delta-opioid receptor mRNA expression and immunohistochemical localization in porcine ileum [9].
  • Selective immunoperoxidase labeling for DOR was detected by light microscopy in NG-108 cells and in the lamina I and II of the dorsal horn of the spinal cord (C2-C4) [1].
  • The following new peptides were prepared and tested for their delta opioid receptor potency and selectivity in the guinea pig ileum assay, the mouse vas deferens assay, and the rat brain binding assay: H-Tyr-D-Pen-Gly-p-NH2Phe-D-Pen-OH (1, [p-NH2Phe4]DPDPE) and H-Tyr-D-Pen-Gly-p-N3Phe-D-Pen-OH (2, [p-N3Phe4]-DPDPE) [10].
  • Using primary antisera directed toward cloned opioid receptors, delta-opioid receptor immunoreactivity was immunohistochemically localized in submucosal neurons and nerve fibers, but immunoreactivities to kappa- or mu-opioid receptors were not detected in the mucosa-submucosa [11].
  • In addition to this phenomenon of morphine, the effects of U50488H and SNC 80 (highly selective delta-opioid receptor agonist) were studied in vitro on mice vas deferens (MVD) of cholestatic animals 2, 5, 7, 10, and 15 days after bile duct ligation [12].

Associations of OPRD1 with chemical compounds


Other interactions of OPRD1


Analytical, diagnostic and therapeutic context of OPRD1


  1. Ultrastructural immunolabeling shows prominent presynaptic vesicular localization of delta-opioid receptor within both enkephalin- and nonenkephalin-containing axon terminals in the superficial layers of the rat cervical spinal cord. Cheng, P.Y., Svingos, A.L., Wang, H., Clarke, C.L., Jenab, S., Beczkowska, I.W., Inturrisi, C.E., Pickel, V.M. J. Neurosci. (1995) [Pubmed]
  2. Potentiation of anaphylaxis in guinea pig ileal mucosa by a selective delta-opioid receptor agonist. Poonyachoti, S., Brown, D.R. Eur. J. Pharmacol. (1999) [Pubmed]
  3. Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid receptor ligands. Calderon, S.N., Rice, K.C., Rothman, R.B., Porreca, F., Flippen-Anderson, J.L., Kayakiri, H., Xu, H., Becketts, K., Smith, L.E., Bilsky, E.J., Davis, P., Horvath, R. J. Med. Chem. (1997) [Pubmed]
  4. The molecular basis of opioid receptor function. Simonds, W.F. Endocr. Rev. (1988) [Pubmed]
  5. Dynorphin is a specific endogenous ligand of the kappa opioid receptor. Chavkin, C., James, I.F., Goldstein, A. Science (1982) [Pubmed]
  6. Dermenkephalin (Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2): a potent and fully specific agonist for the delta opioid receptor. Amiche, M., Sagan, S., Mor, A., Delfour, A., Nicolas, P. Mol. Pharmacol. (1989) [Pubmed]
  7. Characterization of specific delta-opioid binding sites in the distal small intestine of swine. Townsend, D., Brown, D.R. Eur. J. Pharmacol. (2003) [Pubmed]
  8. Hibernation-induction trigger. II. In vitro effects of prairie dog plasma albumin on mouse vas deferens contractility. Bruce, D.S., Cox, D.E., Crane, S.K., Denholm, M.L., Dhyanchand, R.J., Hampl, M.J., Kary, J.A., Krober, A.S., Oeltgen, P.R., Horton, N.D., Harlow, H.J. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  9. Delta-opioid receptor mRNA expression and immunohistochemical localization in porcine ileum. Brown, D.R., Poonyachoti, S., Osinski, M.A., Kowalski, T.R., Pampusch, M.S., Elde, R.P., Murtaugh, M.P. Dig. Dis. Sci. (1998) [Pubmed]
  10. Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group. Landis, G., Lui, G., Shook, J.E., Yamamura, H.I., Burks, T.F., Hruby, V.J. J. Med. Chem. (1989) [Pubmed]
  11. Pharmacological evidence for a 7-benzylidenenaltrexone-preferring opioid receptor mediating the inhibitory actions of peptidic delta- and mu-opioid agonists on neurogenic ion transport in porcine ileal mucosa. Poonyachoti, S., Portoghese, P.S., Brown, D.R. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  12. Subsensitivity to opioids is receptor-specific in isolated guinea pig ileum and mouse vas deferens after obstructive cholestasis. Dehpour, A.R., Rastegar, H., Jorjani, M., Roushanzamir, F., Joharchi, K., Ahmadiani, A. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  13. Topographically designed analogues of [D-Pen,D-Pen5]enkephalin. Hruby, V.J., Toth, G., Gehrig, C.A., Kao, L.F., Knapp, R., Lui, G.K., Yamamura, H.I., Kramer, T.H., Davis, P., Burks, T.F. J. Med. Chem. (1991) [Pubmed]
  14. N,N-dialkylated leucine enkephalins as potential delta opioid receptor antagonists. Lovett, J.A., Portoghese, P.S. J. Med. Chem. (1987) [Pubmed]
  15. Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity. Toth, G., Russell, K.C., Landis, G., Kramer, T.H., Fang, L., Knapp, R., Davis, P., Burks, T.F., Yamamura, H.I., Hruby, V.J. J. Med. Chem. (1992) [Pubmed]
  16. Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands. Rew, Y., Malkmus, S., Svensson, C., Yaksh, T.L., Chung, N.N., Schiller, P.W., Cassel, J.A., DeHaven, R.N., Taulane, J.P., Goodman, M. J. Med. Chem. (2002) [Pubmed]
  17. Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile. Tourwé, D., Mannekens, E., Diem, T.N., Verheyden, P., Jaspers, H., Tóth, G., Péter, A., Kertész, I., Török, G., Chung, N.N., Schiller, P.W. J. Med. Chem. (1998) [Pubmed]
  18. Structure-activity relationships for SNC80 and related compounds at cloned human delta and mu opioid receptors. Knapp, R.J., Santoro, G., De Leon, I.A., Lee, K.B., Edsall, S.A., Waite, S., Malatynska, E., Varga, E., Calderon, S.N., Rice, K.C., Rothman, R.B., Porreca, F., Roeske, W.R., Yamamura, H.I. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  19. Bidirectional effects of endogenous opioid peptides on endothelin release rates in porcine aortic endothelial cell culture: mediation by delta opioid receptor and opioid receptor antagonist-insensitive mechanisms. Arendt, R.M., Schmoeckel, M., Wilbert-Lampen, U., Plasse, A., Heucke, L., Werdan, K. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  20. Prenatal cocaine raises mu-opioid receptor density in piglet cardiorespiratory medulla. Moss, I.R., Laferrière, A. Neurotoxicology and teratology. (2000) [Pubmed]
  21. Delta-opioid receptor activation mimics ischemic preconditioning in the canine heart. Peart, J.N., Patel, H.H., Gross, G.J. J. Cardiovasc. Pharmacol. (2003) [Pubmed]
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