Functional selectivity and classical concepts of quantitative pharmacology.

  title={Functional selectivity and classical concepts of quantitative pharmacology.},
  author={Jonathan D Urban and William P Clarke and Mark von Zastrow and David E. Nichols and Brian K. Kobilka and Harel Weinstein and Jonathan A. Javitch and Bryan L. Roth and Arthur Christopoulos and Patrick M. Sexton and Keith J. Miller and Michael Spedding and Richard B. Mailman},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={320 1},
The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century, yet recent data have revealed that many ligands can differentially activate signaling pathways mediated via a single G protein-coupled receptor in a manner that challenges the traditional definition of intrinsic efficacy. Some terms for this phenomenon include functional selectivity, agonist-directed trafficking, and biased agonism. At the extreme, functionally selective ligands may be both agonists and… CONTINUE READING
Highly Influential
This paper has highly influenced 22 other papers. REVIEW HIGHLY INFLUENTIAL CITATIONS
Recent Discussions
This paper has been referenced on Twitter 1 time over the past 90 days. VIEW TWEETS


Publications citing this paper.
Showing 1-10 of 384 extracted citations


Publications referenced by this paper.
Showing 1-10 of 112 references

Similar Papers

Loading similar papers…