Abstract
Although the opioid peptide dynorphin contains the pentapeptide Leu-enkephalin as its amino-terminal sequence1, the two opioid peptides differ in their potency and sensitivity to antagonism by the specific opiate antagonist naloxone. In the guinea pig myenteric plexus–longitudinal muscle assay, dynorphin(1–13) is 700 times more potent and 13 times less sensitive to naloxone antagonism than Leu-enkephalin1. We have identified the specific amino acids in the dynorphin(6–13) sequence responsible for this higher potency2. One explanation for the difference in naloxone sensitivities is that dynorphin and Leu-enkephalin act through different types of opiate receptors, as first suggested by Goldstein et al.1. This hypothesis has been strongly supported by recent results3 showing that vasa deferentia of mice infused with both D-Ala2-D-Leu5-enkephalin (DADLE) and the opiate alkaloid sulfentanil become tolerant to the effects of Leu-enkephalin and sulfentanil, whereas sensitivity to dynorphina(1–13) remains unchanged. Here we report that the guinea pig ileum myenteric plexus contains two physically distinct classes of opiate receptors: the μ receptor, with which leu-enkephalin (or normorphine) interacts, and a separate dynorphin receptor.
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References
Goldstein, A., Tachibana, S., Lowney, L. I., Hunkapiller, M. & Hood, L. Proc. natn. Acad. Sci. U.S.A. 76, 6666–6670 (1979).
Chavkin, C. & Goldstein, A. Soc. Neurosci. Abstr. 6, 617 (1980).
Wuster, M., Schulz, R. & Herz, A. Neurosci. Lett. 20, 79–83 (1980).
Portoghese, P. S., Larson, D. L., Jiang, J. B., Caruso, T. P. & Takemori, A. E. J. med. Chem 22, 168–173 (1979).
Caruso, T.P., Larson, D. L., Portoghese, P. S. & Takemori, A. E. J. Pharmac. exp. Ther. 213, 539–544 (1980).
Schulz, R. & Goldstein, A. Br. J. Pharmac. 48, 655–666 (1973).
Goldstein, A., Aronow, L. & Kalman, S. M. Principles of Drug Action, 82–104 (Wiley, New York, (1974).
Rocha e Silva, M. Eur. J. Pharmac. 6, 294–302 (1969).
Creese, I. & Snyder, S. H. J. Pharmac. exp. Ther. 194, 205–219 (1975).
Kosterlitz, H. W. & Paterson, S. J. Proc. R. Soc. B210, 113–122 (1980).
Robson, L. E. & Kosterlitz, H. W. Proc. R. Soc. B205, 425–432 (1979).
Smith, J. R. & Simon, E. J. Proc. natn. Acad. Sci. U.S.A. 77, 281–284 (1980).
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Chavkin, C., Goldstein, A. Demonstration of a specific dynorphin receptor in guinea pig ileum myenteric plexus. Nature 291, 591–593 (1981). https://doi.org/10.1038/291591a0
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DOI: https://doi.org/10.1038/291591a0
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