Abstract
The existence of cell membrane-bound sites specific for the binding of opiate narcotic analgesics was demonstrated in 1973 by the laboratories of Simon et al. (1973), Terenius (1973), and Pert and Snyder (1973). The binding of radiolabeled opiate agonists and antagonists is saturable, reversible, and of high affinty (10-10-10-7M) for drugs that exhibit opiate activity. Furthermore, opiate binding correlates well with pharmacological activity. Considerable evidence has been accumulated suggesting that these binding sites are relevant to the pharmacological activity of opiates and are, therefore, part of the receptors for these drugs. The discovery of endogenous peptides with opiate-like (opioid) activity has resulted in the hypothesis that opiate receptors are the receptor sites for these endogenous peptides. They have, therefore, been renamed opioid receptors to suggest their true function.
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Gioannini, T.L., Simon, E.J. (1990). Purification of Opioid Binding Proteins. In: Litwack, G. (eds) Receptor Purification. Receptor Purification, vol 1. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-4612-0461-9_5
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DOI: https://doi.org/10.1007/978-1-4612-0461-9_5
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