The existence of opioid receptors (OR) was postulated in 1954 (Beckett and Casy 1954), at a time when evidence for specific drug-responsive substances was evasive and the concept of biochemical receptors was still in its infancy. Unequivocal confirmation of specific binding sites for opioids in the brain was first reported in 1973 (Pert and Snyder 1973; Simon et al. 1973; Terenius 1973). This breakthrough was shortly followed by evidence that opioid ligands bind specifically to different anatomical locations and show different pharmacological activity, suggesting that several types of opioid receptors exist (Martin et al. 1976; Lord et al. 1977). Based on extensive pharmacological and animal...
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