Testing for inverse agonism with constitutive receptor systems.

This unit discusses the use of constitutive 7-transmembrane/G protein coupled receptor (7TM/GPCR) activity for screening new drug entities. Following an introduction to constitutive 7TM/GPCR activity, the unit centers on the three basic components of a constitutive screening system: the receptor, the receptor coupling components (G protein), and the response reporting system. The design of specific assays to detect inverse agonism and the application of such systems to drug screening are also discussed. Finally, the relative advantages and disadvantages of inverse agonists as therapeutic agents are considered.