Abstract
The identification of opioid receptor involvement in functional endpoints such as antinociception has depended, to a large degree, on the development and availability of ligands with sufficient selectivity to insure confidence that the measured effect is related to activity at the receptor in question. The development of selective ligands has recently progressed at a rapid pace so that a reasonable degree of confidence now exists that in the opioid system, as in many other receptor systems, multiple receptor involvement in most functional endpoints is the rule, rather than the exception. The importance of selective ligands in our understanding of opioid pharmacology has been demonstrated since the early studies of Portoghese (1965) as well as those of Martin and colleagues (Martin 1967; Martin et al. 1976; Gilbert and Martin 1976). These investigators used several opiate agonists in the evaluation of opiate effects in vivo. In particular, the latter group (Martin et al. 1976) used these opiates to establish a profile of responses in their model and provided the basis for an initial classification of opiate receptors which has been remarkably consistent since that time. In this classification, opiate receptors were postulated on the basis of the spectrum of activity produced by several prototype drugs, resulting in the suggestion of opiate μ-receptors which were activated by morphine, κ-receptors acted upon by ketocyclazocine and σ-receptors acted upon by SKF 10047.
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Porreca, F., Burks, T.F. (1993). Supraspinal Opioid Receptors in Antinociception. In: Herz, A., Akil, H., Simon, E.J. (eds) Opioids II. Handbook of Experimental Pharmacology, vol 104 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-77540-6_2
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DOI: https://doi.org/10.1007/978-3-642-77540-6_2
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