Contents

Abstract 160

9.1 Introduction 160

9.2 Source Material and Assay Diversity 160

9.3 High Throughput Screening 161

9.4 Receptor Binding Assays: General Considerations 163

9.4.1 Heterogeneous Receptor Binding Assays 163

9.4.2 Homogeneous Receptor Binding Assays 164

9.4.2.1 Homogeneous Radioactive Binding Assays 164

9.4.2.2 Homogeneous Non-Radioactive Binding Assays 165

9.5 Functional GPCR Assays 167

9.5.1 GTP Binding Assays 168

9.5.2 cAMP Assays 169

9.5.2.1 General Principles of cAMP Assays Identifying

Active Compounds 170

9.5.2.2 Antibody-Dependent cAMP Detection Assays 170

9.5.2.3 Antibody-Free Methods for Measuring cAMP 172

9.5.2.4 cAMP Biosensor 173

9.5.3 Intracellular Calcium Assays 176

9.5.4 Inositol-Triphosphate Assays 179

9.5.5 Melanophore-Based Receptor Functional Activity 179

9.6 Inverse Agonists and Constitutive Activities 180

9.7 Microphysiometer Assays 181

9.8 GPCR Internalization and Trafficking 181

9.9 Screening for Modulators of Orphan Receptors 182

9.10 Conclusions 183

References 183

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