Overview of Ligand-Receptor Binding Techniques -- Radioligand Binding in Different Preparations -- [3H]-GABA Binding to GABAA and GABAB Sites on Rat Brain Crude Synaptic Membranes -- Characterization of Imidazoline Receptors by Radioligand Binding -- Radioligand Binding to Solubilized 5-HT3 Receptors -- Solubilized Muscarinic Acetylcholine Receptors from the Rat Myocardium: Pharmacological and Hydrodynamic Characterization -- Radioligand Binding in Intact Cells -- Autoradiography of Peptide Receptors -- Measurement of Brain Gaba-Benzodiazepine Receptor Levels In Vivo Using Emission Tomography -- General Considerations -- Analysis of Binding Data -- Definition of Receptors in Radioligand-Binding Experiments -- The Use of Binding to Study Nonreceptor Sites -- Autoradiography of Enzymes, Second Messenger Systems, and Ion Channels -- Whole Human Brain Autoradiography of Serotonin Re-Uptake Inhibitors -- Measurement of Agonist-Stimulated [35S]GTP?S Binding to Cell Membranes -- mRNA: Detection by In Situ and Northern Hybridization.

In Receptor Binding Techniques, detailed experimental protocols devised by expert practitioners demonstrate the power of radioligand binding for studying a wide variety of receptors. The methods can be applied to G protein-coupled receptors, receptors with integral ion channels, and sites other than receptors, such as guanine nucleotide binding proteins, enzymes, transporters, and mRNA. The individual protocols encompass many different preparations, ranging from solubilized receptors, through membrane preparations, intact cells, and autoradiography in tissue slices, to PET and SPECT analysis of binding in living human brain. Along with the detailed, easily reproducible instructions, the protocols also take into account the problems inherent in the basic binding technique, such as common experimental artifacts and the definition of receptor sites, as well as problems associated with the use of particular ligands and receptor preparations. Receptor Binding Techniques shows clearly how these techniques can be adapted to many different applications and fully utilized in drug discovery programs. It will be of high value not only to researchers new to the field of receptor binding, but also to more experienced workers, serving as an authoritative bench manual replete with optimalized practical methods and protocols. Pharmacologists, neuroscientists, cell biologists, molecular biologists, and biochemists.