Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation

Trends Pharmacol Sci. 1996 Aug;17(8):280-3. doi: 10.1016/0165-6147(96)10034-1.


Allosteric modulation of a receptor may be proved experimentally by demonstrating an altered radioligand dissociation in the presence of the allosteric modulator. Two-point kinetic experiments provide a screening-type approach to determine the delay of radioligand dissociation caused by allosteric modulation. In this article, Evi Kostenis and Klaus Mohr describe a pitfall in the data analysis that may lead to a suboptimum determination of the allosteric potency in the case of monophasic dissociations, and suggest how this problem may be resolved.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Regulation
  • Humans
  • Kinetics
  • Mathematical Computing
  • Radioligand Assay*
  • Receptors, Drug / drug effects
  • Receptors, Drug / metabolism*


  • Receptors, Drug