Abstract
Of the peptide receptors examined, the opioid receptors are by far the most intensely studied and best characterized systems in the CNS. They consist of at least three receptor types, referred to as JI, 8, and K, and have distinct anatomical distributions (Mansour et al. 1987, 1988; Sharif and Hughes 1988; Tempel and Zukin 1987), ligand selectivities (goldstein and Naidir 1989; James and Goldstein 1984; Robson et al. 1983), and functions in the brain and periphery (Martin 1984; Wood 1982). With their first demonstration nearly 20 years ago (Pert and Snyder 1973; Simon et al. 1973; Terenius 1973), they heralded a new era in the neurosciences, paving the way for the eventual discovery of the opioid peptides and serving as model systems for peptidergic transmission. While the biochemical demonstration of opioid receptors took place in the 1970s, a wealth of pharmacological evidence in the preceding decades had suggested the existence of specific binding sites for the opiates (Beckett and Casey 1954; Portoghese 1965; Woods 1956). The characterization of opiate antagonists, such as naloxone and the stereoselective requirements of opiate agonists, clearly pointed to the existence of opioid receptors prior to the first receptor-binding assay.
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Mansour, A., Watson, S.J. (1993). Anatomical Distribution of Opioid Receptors in Mammalians: An Overview. In: Herz, A., Akil, H., Simon, E.J. (eds) Opioids. Handbook of Experimental Pharmacology, vol 104 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-77460-7_5
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