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Opioid Analgesics pp 445–502Cite as

Opioid Receptors: Facts and Speculations

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Abstract

Opioid receptors were originally conceived as specific sites in the CNS that form a crucial link in the mechanism of pain perception and that fail to function in this respect when bound to certain ligands termed analgesics or analgetics. Substances that block the action of such opioid agonists ligands in a competitive manner were termed opioid antagonists and the two classes of ligand were assumed to compete for the same receptor. Up to the early 1970s there was no direct evidence of opioid receptors; speculations on their existence rested upon classical pharmacology (specificity of action and structure activity analyses, especially stereochemical, of agonists) and the identification of specific antagonists. Over the last 10 years or so, however, the application of radioactive labeled ligands to binding studies and autoradiography has yielded a large body of direct evidence and provided information about the location and general chemical nature of the receptors. Complementary to this evidence and of crucial support to the existence of opioid receptors was, undoubtedly, the discovery and identification of endogenous ligands (enkephalins, endorphins, etc.) since it was inconceivable that such receptors should have evolved on the off chance of interactions with exogenous ligands.

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  1. University of Bath, Bath, UK

    Alan F. Casy & Robert T. Parfitt

  2. Canberra College of Advanced Education, Belconnen, ACT, Australia

    Robert T. Parfitt

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Casy, A.F., Parfitt, R.T. (1986). Opioid Receptors: Facts and Speculations. In: Opioid Analgesics. Springer, Boston, MA. https://doi.org/10.1007/978-1-4899-0585-7_13

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