Opioid Receptors: Cellular and Molecular Mechanisms Underlying Opioid Receptor Function
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 model studies that followed, opioid receptors were originally classed in four types: mu (μ), kappa (κ), sigma (σ) and delta (δ). They were named after specific ligands used for...
- Anton RF, Oroszi G, O'Malley S, Couper D, Swift R, Pettinati H, Goldman D. An evaluation of mu-opioid receptor (OPRM1) as a predictor of naltrexone response in the treatment of alcohol dependence: results from the Combined Pharmacotherapies and Behavioral Interventions for Alcohol Dependence (COMBINE) study. Arch Gen Psychiatry. 2008;65:135–44.PubMedCrossRefGoogle Scholar
- Flicek P, Amode MR, Barrell D, Beal K, Brent S, Chen Y, Clapham P, Coates G, Fairley S, Fitzgerald S, Gordon L, Hendrix M, Hourlier T, Johnson N, Kähäri A, Keefe D, Keenan S, Kinsella R, Kokocinski F, Kulesha E, Larsson P, Longden I, McLaren W, Overduin B, Pritchard B, Riat HS, Rios D, Ritchie GR, Ruffier M, Schuster M, Sobral D, Spudich G, Tang YA, Trevanion S, Vandrovcova J, Vilella AJ, White S, Wilder SP, Zadissa A, Zamora J, Aken BL, Birney E, Cunningham F, Dunham I, Durbin R, Fernández-Suarez XM, Herrero J, Hubbard TJ, Parker A, Proctor G, Vogel J, Searle SM. Ensembl 2011. Nucleic Acids Res. 2011;39:D800–6.PubMedCrossRefGoogle Scholar