Summary
There is ample evidence from studies of peripheral isolated organs, binding of opiate receptor ligands to brain membranes and behavioural experiments that opiate receptors are not homogeneous but consist of different types such as the μ- (= morphine), δ- (= enkephalin), ϰ- (= ketocyclazocine) and the ε- (= β-endorphin) receptors. In addition, there are indications for subtypes within the particular classes of receptors, at least in the case of μ-land ϰ-receptors. In one organ or particular brain structure, several types of receptors can be present—though big differences in the relative concentrations between various brain areas exist. The precise nature of the relationship between the multiplicity of opiate receptors and the multiplicity of endogenous opioids is not clear. The enkephalins and dynorphin appear to be, however, related to, respectively, δ- and ϰ-receptors. According to our present knowledge, there is no strict relationship between certain physiological functions (or pharmacological actions) and the activation of a particular receptor type; for example, μ-, δ- and ϰ-receptors are involved in pain modulation.
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References
Bowen, W. D., Gentleman, S., Herkenham, M., Pert, C. B.: Interconventing my and delta forms of the opiate receptor in the rat striatal patches. Proc. Natl. Acad. Sci. U.S.A. 78, 4818–4822 (1981).
Chang, K.J., Cuatrecasas, P.: Multiple opiate receptors: enkephalins and morphine bind to receptors of different specificity. J. Biol. Chem. 254, 2610–2618 (1979).
Chang, K.J., Hazum, L., Cuatrecasas, P.: Novel opiate binding sites, selective for benzomorphan drugs. Proc. Natl. Acad. Sci. U.S.A. 78, 4141–4145 (1981).
Chavkin, Ch., James, I. F., Goldstein, A.: Dynorphin is a specific endogenous ligand of the x-opioid receptor. Science 215, 413–415 (1982).
Fields, H.L., Emson, P. C., Leigh, B. K., Gilbert, R.F. T., Iversen, L.L.: Multiple opiate receptors in primary afferent fibres. Nature 284, 351–353 (1980).
Kosterlitz, H.A. W., Paterson, S.J., Robson, L.E.: Characterization of the x-subtype of the opiate receptor in the guinea pig brain. Brit. J. Pharmacol. 73, 939–949 (1981).
Leslie, F. M., Chavkin, C., Cox, B. M.: Opioid binding properties of brain and peripheral tissue: Evidence for heterogeneity in opioid ligand binding sites. J.Pharmacol. exp. Ther. 214, 395–402 (1980).
Lord, J. A., Waterfield, A.A., Hughes, J., Kosterlitz, H. W.: Endogenous opioid peptides: multiple agonists and receptors. Nature 267, 495–499 (1977).
Martin, W.R., Eades, C. G., Thompson, J. A., Huppler, R. E., Gilbert, P.E.: The effects of morphine- and nalorphine-like drugs in the nondependent and the morphine-dependent chronic spinal dog. J.Pharmacol. exp. Ther. 197, 517–532 (1976).
Oka, T., Negishi, K., Suda, M., Matsumiya, T., Inazu, T., Ueki, M.: Rabbit vas deferens: A specific bioassay for opioid x-receptors. Europ. J. Pharma-col. 73, 235–236 (1980).
Pasternak, G. W., Childers, S. R., Snyder, S. H.: Opiate analgesia: Evidence for mediation by a subpopulation of opiate receptors. Science 208, 514–515 (1980).
Pfeiffer, A., Herz, A.: Demonstration and distribution of an opiate binding site in rat brain with high affinity for ethylketocyclazocine and SKF 10,047. Biochem. Biophys. Res. Comm. 101, 38–44 (1981).
Pfeiffer, A., Pasi, A., Mehraein, P., Herz, A.: A subclassification of x-sites in human brain by use of dynorphin. Neuropeptides 2, 89–97 (1981).
Pfeffer, A., Herz, A.: Discrimination of 3 opiate binding sites with the use of a computerized curve fitting technique. Molec. Pharmacol. 21, 266–271 (1982).
Pfeiffer, A., Pasi, A., Mehraein, P., Herz, A.: Opiate receptor binding sites in human brain. Brain Res. 248, 87–96 (1982).
Schulz, R., Wüster, M., Krenss, H., Herz, A.: Selective development of tolerance without dependence in multiple opiate receptors of mouse vas deferens. Nature 285, 242–243 (1980).
Schulz, R., Wüster, M., Krenss, H., Herz, A.: Lack of crosstolerance on multiple opiate receptors in the mouse vas deferens. Molec. Pharmacol. 18, 395–401 (1980).
Schulz, R., Wüster, M.: Are there subtypes (isoreceptors) of multiple opiate receptors in the mouse vas deferens? Europ. J. Pharmacol. 76, 61–66 (1981).
Schulz, R., Wüster, M., Herz, A.: Pharmacological characterization of the c-opiate receptor. J. Pharmacol. exp. Ther. 216, 604–606 (1981).
Schulz, R., Wüster, M., Rubini, P., Herz, A.: Functional opiate receptors in the guinea-pig ileum: their differentiation by means of selective tolerance development. J. Pharmacol. exp. Ther. 219, 547–550 (1981).
Schulz, R., Wüster, M., Herz, A.: Differentiation of opiate receptors in the brain by selective development of tolerance. Pharmacol. Biochem. Behay. 14, 75–79 (1981).
Shearman, G. T., Herz, A.: Evidence that the different discriminative stimulus properties of fentanyl and ethylketocyclazocine in the rat are mediated by an interaction with different opiate receptors. J. Pharmacol. exp. Ther. 221, 735–739 (1982).
Shearman, G. T., Herz, A.: D-Ala2, D-Leu5-Enkephalin generalizes to a discriminative stimulus produced by fentanyl but not ethylketocyclazocine. Pharmacol. Biochem. Behay. 16, 249–252 (1982).
Snyder, S. H., Goodman, R. R.: Multiple neurotransmitter receptors. J. Neuro-chem. 35, 5–15 (1980).
Upton, N., Sewell, W., Spencer, P. S.: Differentiations of potent µ- and x-opiate agonists using heat and pressure antinociceptive profiles and combined potency analgesia. Europ. J. Pharmacol. 78, 421–429 (1982).
Vaught, J. L., Kitano, T., Takemori, A. E.: Interactions of leucine-enkephalin and narcotics with opioid receptors. Mol. Pharmacol. 19, 236–241 (1981).
Williams, J., Zieglgänsberger, W.: Neurones in the frontal cortex of the rat carry multiple opiate receptors. Brain Res. 226, 304–308 (1981).
Wood, P. L.: Commentary. Multiple opiate receptors: support for unique my, delta and kappa sites. Neuropharmacology 21, 487–497 (1982).
Wood, P. L., Rackham, A., Richard, J.: Spinal analgesia: comparison of the my agonist morphine and the x-agonist ethylketocyclazocine. Life Sci. 28, 2119–2135 (1981).
Wüster, M., Schulz, R., Herz, A.: Highly specific opiate receptors for dynorphin (1–13) in the mouse vas deferens. Europ. J. Pharmacol. 62, 235–236 (1980).
Wüster, M., Schulz, R., Herz, A.: Multiple opiate receptors in peripheral tissue preparations. Biochem. Pharmacol. 30, 1883–1887 (1981).
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Herz, A. (1983). Multiple Opiate Receptors and Their Functional Significance. In: Goldstein, M., Jellinger, K., Riederer, P. (eds) Basic Aspects of Receptor Biochemistry. Journal of Neural Transmission, vol 18. Springer, Vienna. https://doi.org/10.1007/978-3-7091-4408-4_21
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DOI: https://doi.org/10.1007/978-3-7091-4408-4_21
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