Characterization of Receptors by Radiolabeled Ligand-Binding Techniques

Radio&and binding is one of the most widely used techniques by which the pharmacological and biochemical properties of receptors are determined. This technique was used in many of the pioneering studies of the receptors for hormones, neurotransmitters, and drugs and is now routinely used by laboratories throughout the world The underlying principle of the approach is fairly simple; by isotopically labeling a ligand, its interaction with a receptor can be directly monitored, thus allowing information about the properties of the receptor to be gathered. Use of the appropriate radioligand binding methodology can provide many insights into the characteristics of the receptor being studied, from the determination of binding constants of radioligands to the construction of complex models that explain the molecular mechanisms by which ligand-receptor interactions occur.