Partial agonists and G protein-coupled receptor desensitization.

  title={Partial agonists and G protein-coupled receptor desensitization.},
  author={Richard B. Clark and Brian J. Knoll and Rachael Barber},
  journal={Trends in pharmacological sciences},
  volume={20 7},
Weak or partial agonists induce less desensitization of G protein-coupled receptors (GPCRs) than do strong agonists. However, there have been few attempts to relate partial agonism quantitatively with the various parameters of agonist-induced desensitization, and to elucidate the mechanisms involved. Our understanding of how the treatment of cells and tissues with partial agonists affects their capacity to activate receptors is based on continued progress in defining partial agonism and the… CONTINUE READING