UNIT 1.3 Practical Aspects of Radioligand Binding

  1. Michael McKinney

Published Online: 1 MAY 2001

DOI: 10.1002/0471141755.ph0103s00

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

McKinney, M. 2001. Practical Aspects of Radioligand Binding. Current Protocols in Pharmacology. 1:1.3.

Author Information

  1. Mayo Clinic Jacksonville, Jacksonville, Florida

Publication History

  1. Published Online: 1 MAY 2001
  2. Published Print: MAR 1998

This is not the most recent version of the article. View current version (1 JUL 2006)


Radioligand binding assays can be used to characterize receptors in their natural environment (wild type) as well as those transfected into cell lines. They can be used to study receptor dynamics and localization, to identify novel chemical structures that interact with receptors, and to define ligand activity and selectivity. The technique thus serves as a valuable adjunct to other pharmacological and molecular biological approaches. This unit describes the major issues involved in developing a binding assay, such as selecting a radioligand, tissue preparation, optimization of assay parameters, and separation of bound from free ligand. Methods for analysis of the binding data are carefully considered, and tips for troubleshooting a binding assay are also provided.