Overview of receptor interactions of agonists and antagonists

Current Protocols in Pharmacology
Terry Kenakin


Historically, the earliest methods used to quantitatively measure the fundamental properties of drugs (namely affinity and efficacy) employed isolated tissues, and it is in this realm that the null methods used to define "receptor pharmacology" were described. This unit describes these methods and their use to specifically classify agonists (through potency ratios and determination of relative affinities and efficacies) and antagonists (through analysis of surmountable and insurmountable antagonism) to yield estimates of potency. Different drugs can yield different behaviors in various tissues, so this unit is centered on a flow diagram to indicate the type of analysis appropriate for the behavior observed. For example, some agonists may be full agonists in some tissues and partial agonists in others, while some antagonists may demonstrate surmountable simple competitive antagonism in some tissues and insurmountable non-competitive antagonism in others. Methods exist for determination of affinity and efficacy for all of these behaviors, and these are delineated in this unit.


Jan 1, 1985·Journal of Cardiovascular Pharmacology·Terry Kenakin
Dec 22, 1983·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·J W Black, P Leff
Mar 1, 1982·Canadian Journal of Physiology and Pharmacology·Terry Kenakin
May 31, 2002·Pharmacological Reviews·A Christopoulos, Terry Kenakin
Dec 1, 1956·British Journal of Pharmacology and Chemotherapy·R P STEPHENSON
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Aug 24, 1965·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·W D PATON, H P RANG
Jan 1, 1955·Quarterly Journal of Experimental Physiology and Cognate Medical Sciences·J H GADDUMF F STEPHENS
Jan 1, 1950·Biochimica Et Biophysica Acta·H A KREBS
Jul 22, 2006·The Journal of Pharmacology and Experimental Therapeutics·Terry KenakinChristian Watson
Sep 1, 1949·British Journal of Pharmacology and Chemotherapy·H O SCHILD


Mar 21, 2017·European Journal of Pharmacology·Martin HennenbergChristian Gratzke
Mar 27, 2018·British Journal of Pharmacology·Qingfeng YuMartin Hennenberg
Sep 1, 2017·American Journal of Physiology. Renal Physiology·Annika HerlemannMartin Hennenberg
Jan 6, 2011·Microbiology and Immunology·Aya Fukui-MiyazakiYasuhiko Horiguchi
Nov 5, 2010·Current Protocols in Toxicology·Cristina Pozzoli, Enzo Poli

Related Concepts

Dose-Response Relationship, Drug
Drug Antagonism
Receptors, Drug
Tissue Culture Techniques
Drug Agonism

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