TIPS review
Binding selectivity profiles for ligands of multiple receptor types: Focus on opioid receptors

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Abstract

The aim of radioreceptor assays for multiple types of binding sites is to study and characterize one without interference from another i.e., to ‘isolate’ (operationally) a single type of site. Although Scatchard analysis and data fitting by computer can be useful at the outset in establishing parameters of the primary (highest-affinity, preferred) sites, they are of limited value for secondary (lower-affinity, nonpreferred) sites. What is required is the exclusive labeling of each type of site in order to obtain binding constants for an array of competing ligands, and thus to characterize the ligands quantitatively and to establish the unique identities of the binding sites. A binding site is described by a unique Binding Site Signature the quantitative rank order of affinities of a large set of competing ligands. The selectivity of a ligand is described quantitatively by a Binding Selectivity Profile (BSP), the set of decimal logarithms of the binding constants at each site. Avram Goldstein illustrates the method of depicting BSP for ligands that are selective for μ, enkephalin (δ), and dynorphin (κ) opioid binding sites.

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