Abstract
Previous work from this laboratory suggests that distinct morphine and enkephalin receptors coexist in an opioid receptor complex. In this paper the interaction of naloxone with the receptor complex is studied. The results further strengthens the hypothesis that leucine enkephalin binds poorly to the morphine receptor and that morphine and enkephalin receptors are allosterically coupled.
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Lord, J. A. H., Waterfield, A. A., Hughes, J., andKosterlitz, H. W. 1977. Endogenous opioid peptides: multiple agonists and receptors. Nature 267:495–499.
Chang, K. J., andCuatrecacas, P. 1979. Multiple opiate receptors. J. Biol. Chem. 254:2620–2618.
Chang, K. J., Cooper, B. R., Hazum, E., andCuatrecacas, P. 1979. Multiple opiate receptors: different regional distribution in the brain and differential binding of opiates and opioid peptides. Mol. Pharmacol. 16:91–104.
Law, P., andLoh, H. H. 1978.3H-leu5-enkephalin specific binding to synaptic membranes: comparison with [3H]dihydromorphine and [3H]naloxone. Res. Comm. Chem. Path. Pharmacol. 21:409–434.
Simantov, R., Childers, S. R., andSnyder, S. H. 1978. The opiate receptor binding interaction of [3H]methionine enkephalin, an opioid peptide. Eur. J. Pharmacol. 47:319–331.
Kosterlitz, H. W., andPaterson, S. J. 1980. Characterization of opioid receptors in nervous tissue. Proc. R. Soc. Lond. 210:113–122.
Goodman, R. R., Snyder, S. H., Kuhar, M. J. andYoung, W. S., III 1980. Differentiation of delta and mu opiate receptor localization by light microscopic autoradiography. Proc. Natl. Acad. Sci. USA 77:6239–6243.
Pert, C. B., Taylor, D. P., Pert, A., Herkenham, M. andKent, J. L. 1980. Neural Peptides and Neuronal Communication Pages 581–589.in E. Costa andM. Trabucci (eds.) Raven Press, New York.
Herkenham, M., andPert, C. B. 1980. In vitro autoradiography of opiate receptors in rat brain suggests loci of “opiatergic” pathways. Proc. Natl. Acad. Sci. USA 77:5532–5536.
Smith, J. R., andSimon, E. J. 1980. Selective protection of stereospecific enkephalin and opiate binding against inactivation by N-ethylmaleimide: evidence for two classes of opiate receptors. Proc. Natl. Acad. Sci. USA 77:281–284.
Robson, L. E., andKosterlitz, H. W. 1979. Specific protection of the binding sites of D-Ala2-D-Leu5-enkephalin (δ-receptor) and dihydromorphine (μ-receptor). Proc. R. Soc. Lond. 205:425–432.
Schulz, R., Wuster, M., Krenss, H., andHerz, A. 1980. Lack of cross tolerance on multiple opiate receptors in the mouse vas deferens. Mol. Pharmacol. 18:395–401.
Rothman, R. B., andWestfall, T. C. 1982. Morphine allosterically modulates the binding of [3H]leucine enkephalin to a particulate fraction of rat brain. Molec. Pharmacol. 21:538–547.
Rothman, R. B., andWestfall, T. C. 1982. Allosteric coupling between morphine and enkephalin receptors in vitro. Molec. Pharmacol. 21:548–557.
Rothman, R. B., andWestfall, T. C. 1981. Allosteric modulation by leucine enkephalin of [3H]naloxone binding in rat brain. Eur. J. Pharmacol. 72:365–368.
Feldman, H. A. 1972. Mathematical theory of complex ligand-binding systems at equilibrium: dome methods of parameter fitting. Anal. Biochem. 48:317–338.
Lee, N. M., andSmith, A. P. 1980. A protein and lipid model of the opiate receptor. Life Sci. 26:1459–1463.
Chang, K. H., Hazum, E., andCuatrecacas, P. 1981. Novel opiate binding sites selective for benzomorphan drugs. Proc. Natl. Acad. Sci. USA 78:4141–4145.
Kosterlitz, H. W., Paterson, S. J., andRobson, L. E. 1981. Characterization of the K-subtype of the opiate receptor in the guinea pig brain. Br. J. Pharmac. 73:939–949.
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Rothman, R.B., Westfall, T.C. Interaction of naloxone with the opioid receptor complex in vitro. Neurochem Res 7, 1375–1384 (1982). https://doi.org/10.1007/BF00966066
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DOI: https://doi.org/10.1007/BF00966066