A μ-opioid receptor-filter assay: Rapid estimation of binding affinity of ligands and reversibility of long-lasting ligand-receptor complexes
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2019, Molecular and Cellular EndocrinologyCitation Excerpt :This method has been applied successfully by ourselves and others to determine the kinetics of both antagonists (Dowling and Charlton, 2006; Stoddart et al., 2018, Sykes et al., 2014a) and agonists (Guo et al., 2012; Sykes et al., 2009; Sykes et al., 2012a) acting at a variety of GPCRs and more recently at non-GPCR targets (Yu et al., 2015). Alternatively, multistep washout experiments (see Vauquelin and Van Liefde., 2012 for a comprehensive review) have been employed to compare the dissociation rates of unlabelled antipsychotics (Leysen and Gommeren, 1984; Tresadern et al., 2011) and mu opoid receptor specific ligands (Ilien et al., 1988) although this method is qualitative and only allows relative differences in dissociation rates to be approximated. When used with high affinity ligands, these type of experiments provide a high degree of sensitivity, nonetheless the use of radioactive ligands as tracers presents a number of challenges.
Uniform assessment and ranking of opioid Mu receptor binding constants for selected opioid drugs
2011, Regulatory Toxicology and PharmacologyCitation Excerpt :Variability in the measured Ki values can be due to the radioligand, tissue source, animal species and strain, and assay methodology. Numerous articles have shown that the radioligand used in the competitive binding assays can result in different Ki values for the same drug (Spetea et al., 2003; Chen et al., 1993; Emmerson et al., 1996; Toll et al., 1998; Ilien et al., 1988; Childers et al., 1979; Nielsen et al., 2007). Because of the variability of the reported binding affinity data for narcotic drugs, our study was designed to develop a compendium of uniformly derived binding constants using commercially available cell membranes expressing human MOR.
Competitive displacement binding assay on rat brain sections and using a β-imager: Application to μ-opioid ligands
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