Development of Novel Irreversible Ligands

Alkylating affinity labels are reactive compounds that bind receptors in a covalent manner. This property makes them useful tools with which to study the structure and function of these important biological recognition molecules. To familiarize investigators with the use of these compounds, an overview of their general properties in terms of design, pharmacology, and chemistry is presented. In addition, some experimental approaches to characterizing their irreversible effects are described. Finally, several uses of alkylating affinity labels for the determination of a receptor reserve, receptor turnover, and studies on receptor structure are briefly outlined. important limitations with the use of these compounds are discussed, and examples focusing mainly on catecholamine receptors are given.