Quantification of cAMP and cGMP analogs in intact cells: pitfalls in enzyme immunoassays for cyclic nucleotides

Naunyn Schmiedebergs Arch Pharmacol. 2011 Aug;384(2):169-76. doi: 10.1007/s00210-011-0662-6. Epub 2011 Jun 29.

Abstract

Immunoassays are routinely used as research tools to measure intracellular cAMP and cGMP concentrations. Ideally, this application requires antibodies with high sensitivity and specificity. The present work evaluates the cross-reactivity of commercially available cyclic nucleotide analogs with two non-radioactive and one radioactive cAMP and cGMP immunoassay. Most of the tested cyclic nucleotide analogs showed low degree competition with the antibodies; however, with Rp-cAMPS, 8-Br-cGMP and 8-pCPT-cGMP, a strong cross-reactivity with the corresponding cAMP and cGMP, respectively, immunoassays was observed. The determined EIA-binding constants enabled the measurement of the intracellular cyclic nucleotide concentrations and revealed a time- and lipophilicity-dependent cell membrane permeability of the compounds in the range of 10-30% of the extracellular applied concentration, thus allowing a more accurate prediction of the intracellular analog levels in a given experiment.

MeSH terms

  • Animals
  • Binding, Competitive
  • Blood Platelets / drug effects
  • Blood Platelets / immunology
  • Blood Platelets / metabolism
  • Blotting, Western
  • CHO Cells
  • Cell Membrane Permeability
  • Cricetinae
  • Cricetulus
  • Cross Reactions
  • Cyclic AMP / analogs & derivatives*
  • Cyclic AMP / analysis*
  • Cyclic AMP / immunology
  • Cyclic GMP / analogs & derivatives*
  • Cyclic GMP / analysis*
  • Cyclic GMP / immunology
  • Electrophoresis, Polyacrylamide Gel
  • Humans
  • Immunoenzyme Techniques / methods*
  • Radioimmunoassay

Substances

  • Cyclic AMP
  • Cyclic GMP