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G Protein-Linked Opioid Receptors

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G Protein Methods and Protocols

Part of the book series: Neuromethods ((NM,volume 31))

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Abstract

Opiates, such as morphine and heroin, exert their pharmacological effects by binding to highly specific receptor proteins on the cell surface of neuronal and nonneuronal cells. In 1973, researchers in three different laboratories demonstrated the presence of receptors specific for opiates in preparations from brain and intestine (Pert and Snyder, 1973; Simon et al., 1973; Terenius, 1973). These studies satisfied the criteria first enunciated by Goldstein et al. (1971) for a narcotic receptor that is specific for the pharmacologically active D(−) enan-tiomer of the narcotics. The existence of specific opiate receptors in brain led many scientists to look for endogenous lig-ands in the brain for which opiate receptors exist. In 1975, Hughes et al. isolated and characterized two pentapeptides (Met- and Leu-enkephalins) from bovine brain that were able to mimic the actions of morphine in the pharmacological test systems. Now, it is known that a family of more than 20 endogenous opioid receptor ligands are generated from three precursor proteins, namely, proopiomelanocortin, proen-kephalin, and prodynorphin (Evans et al., 1988). Based on the pharmacological potency and the selectivity of receptors for various opioid ligands, the receptors were classified into μ, δ, and κ receptors (Pasternak, 1986; Zukin et al., 1988).

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References

  • Ahmed, M. S., Zhou, D. H., Cavinato, A. G., and Maulik, D (1989) Opioid binding properties of the purified kappa receptor from human placenta. Life Set 44, 861–71.

    Article  CAS  Google Scholar 

  • Bidlack, J. M., Abood, L G, Osei-Gyimah, P., and Archer, S. (1981) Purification of opiate receptor from rat brain. Proc. Natl. Acad. Sci. USA 78, 636–639.

    Article  PubMed  CAS  Google Scholar 

  • Blume, A. J., Lichtshtem, D., and Boone, G. (1979) Coupling of the opiate receptors to adenylate cyclase: requirement for Na+ and GTP. Proc. Natl. Acad. Sci. USA 76, 5626–5630

    Article  PubMed  CAS  Google Scholar 

  • Chakrabarti, S., Law, P.-Y, and Loh, H H (1995) Neuroblastoma Neuro 2A cells stably expressing a cloned μ-opioid receptor, a specific cellular model to study acute and chronic effects of morphine Mol. Bram Res 30, 269–278.

    Article  CAS  Google Scholar 

  • Chen, Y, Mestek, A., Liu, J., Hurley, A., and Yu, L. (1993) Molecular cloning and functional expression of a mu opioid receptor from rat brain. Mol. Pharmacol. 44, 8–12.

    PubMed  CAS  Google Scholar 

  • Cho, T M, Ge, B. L, Yamato, C, Smith, A. P., and Loh, H. H. (1983) Isolation of opioid binding components by affinity chromatography and reconstitution of binding activities. Proc. Natl. Acad. Sci. USA 80, 5176–5180.

    Article  PubMed  CAS  Google Scholar 

  • Cho, T. N., Masegawa, J I., Ge, B. L., and Loh, M. M. (1986) Purification to apparent homogeneity of μ type opioid receptor from rat brain. Proc. Natl. Acad. Sci USA 83, 4138–4142.

    Article  PubMed  CAS  Google Scholar 

  • Cruciani, R A., Dvorkin, B., Morris, S A, Crain, S M, and Makman, M H. (1993) Direct coupling of opioid receptors to both stimulatory and inhibitory guanine nucleotide-binding proteins in Fll neuroblastoma sensory neuron hybrid cells. Proc Natl Acad Sci USA 90, 3019–3023.

    Article  PubMed  CAS  Google Scholar 

  • Evans, C, Hammond, D. L., and Frederickson, R C A (1988) The opioid peptides, in The Opiate Receptors (Pasternak, G W, ed.), Humana, Clifton, NJ, pp. 23–74.

    Google Scholar 

  • Evans, J., Keith, J D E., Morrison, H., Magendzo, K., and Edwards, R H. (1992) Cloning of delta opioid receptor by functional expression. Science 258, 1952–1955

    Article  PubMed  CAS  Google Scholar 

  • Frey, E. A. and Kebabian, J. W. (1984) A μ-opiate receptor in 7315c tumor tissue mediates inhibition of immunoreactive prolactin release and adenylate cyclase activity. Endocrinology 115, 1799–1804.

    Article  Google Scholar 

  • Frey, E. A., Gosse, M E, and Cote, T E. (1989) Reconstitution of the solu-bihzed in opioid receptor coupled to a GTP-binding protein. Eur J. Pharmacol. 172, 347–356.

    Article  PubMed  CAS  Google Scholar 

  • Gioannini, T. L., Howard, A. D., Hiller, J. M., and Simon, E J. (1985) Purification of an active opioid binding protein from bovine striatum. J Biol Chem. 260, 15,117–15,121

    PubMed  CAS  Google Scholar 

  • Goldstein, A, Lowney, L I, and Pal, B. K. (1971) Stereospecific and nonspecific interactions of the morphine congener levorphanol in subcel-lular fractions of mouse brain. Proc. Natl. Acad. Sci. USA 68, 1742–1747.

    Article  PubMed  CAS  Google Scholar 

  • Gomathi, G., and Sharma, S. K. (1993) Purification and reconstitution of the δ opioid receptor FEBS Lett. 330, 146–150.

    Article  PubMed  CAS  Google Scholar 

  • Gomes, I., Sharma, P., and Sharma, S. K. (1997) manuscript submitted.

    Google Scholar 

  • Hughes, J., Smith, T. W, Kosterlitz, H W, Fothergill, L. A., and Morris, H. R. (1975) Identification of two related pentapeptides from brain with potent agonist activity. Nature 258, 577–579

    Article  PubMed  CAS  Google Scholar 

  • Jin, W, Lee, N. M., Loh, H H., and Thayer, S. A. (1994) Opioids mobilize calcium from inositol 1,4,6-triphosphate sensitive stores in NG108–15 cells. J Neurosa. 14, 1920–1929.

    CAS  Google Scholar 

  • Kieffer, B. L, Befort, K, Gavenaux-Ruff, C, and Hirth, G. (1992) The delta opioid receptor Isolation of a cDNA by expression cloning and pharmacological characterization. Proc. Natl Acad. Sci. USA 89, 12,048–12,052.

    Article  PubMed  CAS  Google Scholar 

  • Klee, W A and Nirenberg, M. (1974) Aneuroblastoma × glioma hybrid cell line with morphine receptors. Proc. Natl. Acad. Sci. USA 71, 3474–3477

    Article  PubMed  CAS  Google Scholar 

  • Knapp, R. J., Vaughn, L. K., and Yamamura, H I (1995) Selective ligands for μ and δ opioid receptors, in The Pharmacology of Opioid Peptides, (Tseng, L F., ed), Harwood Academic Publishers, Wisconsin, pp 1–27.

    Google Scholar 

  • Koski, G. and Klee, W. A. (1981) Opiates inhibit adenylate cyclase by stimulating GTP hydrolysis. Proc. Natl. Acad. Sci. USA 78, 4185–4189

    Article  PubMed  CAS  Google Scholar 

  • Loh, H. H. and Smith, A P. (1990) Molecular characterization of opioid receptors. Annu. Rev Pharmacol. Toxicol. 30, 123–147

    Article  PubMed  CAS  Google Scholar 

  • Meng, F., Xie, G X, Thompson, R, Mansour, A., Goldstein, A., Watson, S. J., and Akil, H. (1993) Clonmg and pharmacological characterization of rat κ-opioid receptor. Proc. Natl. Acad. Sci. USA 90, 9954–9958.

    Article  PubMed  CAS  Google Scholar 

  • North, R. A. (1989) Drug receptors and the inhibition of nerve cells. Br. J. Pharmacol. 98, 13–28.

    PubMed  CAS  Google Scholar 

  • North, R. A., Williams, J. T, Suprenant, A., and Christie, M. J. (1987) μ and δ receptors belong to a family of receptors that are coupled to potassium channels Proc Natl. Acad. Sct. USA 84, 5487–5491.

    Article  CAS  Google Scholar 

  • Olianas, M. C. and Onali, P (1992) Characterization of opioid receptors mediating stimulation of adenylate cyclase activity in rat olfactory bulb. Mol. Pharmacol. 42, 109–115

    PubMed  CAS  Google Scholar 

  • Palazzi, E, Ceppi, E., Guglielmetti, F, Catozzi, L., Amoroso, D., and Grop-petti, A. (1996) Biochemical evidence of functional interaction between μ and δ opioid receptors in SK-N-BE neuroblastoma cell line. J Neurochem 67, 138–144.

    Article  PubMed  CAS  Google Scholar 

  • Pasternak, G. W (1986) Multiple morphine and enkephalin receptors Biochemical and pharmacological aspects Ann NY Acad. Sci. 467, 130–139

    Article  PubMed  CAS  Google Scholar 

  • Pert, C. B. and Snyder, S. H. (1973) Opiate receptor Demonstration in nervous tissue. Science 179, 1011–1014.

    Article  PubMed  CAS  Google Scholar 

  • Polastron, J., Mur, M, Mazarguil, H, Puget, A., Meunier, J.-C, and Jauzac, P. (1994) SK-N-BE neuroblastoma cell line containing two sub types of δ opioid receptors. J. Neurochem 62, 898–906

    Article  PubMed  CAS  Google Scholar 

  • Porzig, M. (1990) Pharmacological modulation of voltage dependent calcium channels in intact cells Rev Physiol Biochem Pharmacol 114, 209–262.

    Article  PubMed  CAS  Google Scholar 

  • Roerig, S, Loh, H H., and Law, P. Y. (1992) Identification of three separate guanine-nucleotide binding proteins that interact with δ-opioid receptor in NG108-15 neuroblastoma × ghoma hybrid cells. Mol Pharmacol. 41, 822–831

    PubMed  CAS  Google Scholar 

  • Scheideler, M. A. and Zukin, R. S. (1990) Reconstitution of solubihzed delta opioid receptor binding sites in lipid vesicles. J. Biol. Chem. 265, 15,176–15,182

    PubMed  CAS  Google Scholar 

  • Sharma, S. K., Nirenberg, M, and Klee, W. A (1975a) Morphine receptors as regulators of adenylate cyclase activity. Proc. Natl. Acad. Sci. USA 72, 590–594.

    Article  PubMed  CAS  Google Scholar 

  • Sharma, S. K., Klee, W. A., and Nirenberg, M (1975b) Dual regulation of adenylate cyclase accounts for narcotic dependence and tolerance Proc. Nati Acad. Sci. USA 72, 3092–3096

    Article  CAS  Google Scholar 

  • Sharma, S Klee, W A, and Nirenberg, M. (1977) Opiate dependent modulation of adenylate cyclase. Proc. Natl Acad. Sci USA 74, 3365–3369.

    Article  PubMed  CAS  Google Scholar 

  • Simon, E. J., Hiller, J. M., and Edelman, I (1973) Stereospecific binding of the potent narcotic analgesic 3H-etorphine to rat brain homogenate Proc. Natl. Acad. Sci USA 70, 1947–1949.

    Article  PubMed  CAS  Google Scholar 

  • Simon, J., Benyhe, J., Hepp, J., Varga, K, Medzihradsky, K., Borsodi, A, and Wollemann, M. (1990) Method of isolation of kappa-opioid binding sites by dynorphin affinity chromatography J. Neurosci. Res. 25, 549–555

    Article  PubMed  CAS  Google Scholar 

  • Simonds, W. F., Burke, R., Jr, Rice, K. C, Jacobson, A. E, and Klee, W. A. (1985) Purification of the opiate receptor of NG108-15 neuroblas-toma-glioma hybrid cells Proc Nati. Acad. Sei. USA 82, 4974–4978.

    Article  CAS  Google Scholar 

  • Terenius, L. (1973) Stereospecific interaction between narcotic analgesics and a synaphc plasma membrane fraction of rat cerebral cortex Acta. Pharmacol. Toxicol 32, 317–320.

    Article  CAS  Google Scholar 

  • Tsunoo, A., Yoshii, M., and Narahashi, T (1986) Block of calcium channels by enkephalin and somatostatin in neuroblastoma-ghoma hybrid cells. Proc Nati Acad Set. USA 83, 9832–9836

    Article  CAS  Google Scholar 

  • Ueda, H., Harada, H, Nozaki, M., Katada, T, Ui, M, Satoh, M., and Ta-kagi, H (1988) Reconstitution of rat brain opioid receptors with purified guanine nucleotide-binding regulatory proteins, Gi and Go. Proc. Nati. Acad Sci. USA 85, 7013–7017.

    Article  CAS  Google Scholar 

  • Yu, V., Richards, M, L., and Sadee, W. (1986) A human neuroblastoma cell line expresses i and 6 opioid receptor sites. J Biol. Chem. 261, 1065–1070.

    PubMed  CAS  Google Scholar 

  • Zukin, R. Z., Eghlah, M, Olive, D., Unterwald, E. M., and Tempel, A (1988) Characterization and visualization of rat and guinea pig brain opioid receptors: Evidence for and opioid receptors. Proc. Nati. Acad Sa USA 85, 4061–4065.

    Article  CAS  Google Scholar 

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Author information

Authors and Affiliations

  1. Laboratory of Neurochemistry, National Institute of Neurological Disease and Stroke, National Institutes of Health, Bethesda, MD

    Pushkar Sharma

  2. Department af Biochemistry, All lndia Institute of Medical Sciences, New Delhi, India

    Ivone Gomes & Shail K. Sharma

Authors
  1. Pushkar Sharma
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  2. Ivone Gomes
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  3. Shail K. Sharma
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Editor information

Editors and Affiliations

  1. McMaster University, Hamilton, Canada

    Ram K. Mishra

  2. University of Alberta, Edmonton, Canada

    Glen B. Baker

  3. University of Saskatchewan, Saskatoon, Canada

    Alan A. Boulton

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© 1997 Humana Press Inc

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Sharma, P., Gomes, I., Sharma, S.K. (1997). G Protein-Linked Opioid Receptors. In: Mishra, R.K., Baker, G.B., Boulton, A.A. (eds) G Protein Methods and Protocols. Neuromethods, vol 31. Humana Press. https://doi.org/10.1385/0-89603-490-9:207

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  • DOI: https://doi.org/10.1385/0-89603-490-9:207

  • Publisher Name: Humana Press

  • Print ISBN: 978-0-89603-490-7

  • Online ISBN: 978-1-59259-636-2

  • eBook Packages: Springer Protocols

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