Competitive binding studies with multiple sites. Effects arising from depletion of the free radioligand

Biochim Biophys Acta. 1980 Oct 15;632(3):464-9. doi: 10.1016/0304-4165(80)90242-1.

Abstract

Apparently anomalous behaviour arises if a radiolabelled drug and a non-radioactive drug compete for binding to a membrane-bound receptor when (a) there is severe depletion of the radiolabelled drug and (b) the non-radioactive drug binds to a heterogeneous population of binding sites. In extreme cases, binding of the non-radioactive drug to the sites of high affinity can be obscured completely. This phenomenon is illustrated by the binding of carbachol to muscarinic receptors, estimated by inhibition of a radiolabelled antagonist.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive
  • Brain / metabolism
  • Male
  • Models, Biological
  • Radioligand Assay / standards*
  • Rats
  • Receptors, Drug / analysis*

Substances

  • Receptors, Drug