Effect of deuteration on the metabolism and clearance of some pharmacologically active compounds--synthesis and in vitro metabolism of deuterated derivatives of dronedadrone

J Labelled Comp Radiopharm. 2013 Jul-Aug;56(9-10):504-12. doi: 10.1002/jlcr.3090. Epub 2013 Sep 4.

Abstract

The synthesis and in vitro metabolism studies of a family of specifically deuterated derivatives of dronedarone are described. Metabolic stability and clearance of the parent compound are not sensitive to deuterium substitution, irrespective of the position of the heavy label.

Keywords: antiarrhythmic; deuterium; deuterium labelling; in vitro metabolism; isotope effect; stable labelled synthesis.

MeSH terms

  • Amiodarone / analogs & derivatives*
  • Amiodarone / chemical synthesis
  • Amiodarone / chemistry
  • Amiodarone / metabolism
  • Chemistry Techniques, Synthetic
  • Deuterium / chemistry*
  • Dronedarone
  • Hepatocytes / metabolism
  • Humans
  • Structure-Activity Relationship

Substances

  • Deuterium
  • Dronedarone
  • Amiodarone