An admonition when measuring the lipophilicity of radiotracers using counting techniques

Appl Radiat Isot. 2001 Feb;54(2):203-8. doi: 10.1016/s0969-8043(00)00269-4.

Abstract

Log P measurements are a fundamental physico-chemical parameter and one of the cornerstones of structure activity relationships in medicinal chemistry. Despite the attractiveness of the method, the use of counting techniques to measure the log P of lipophilic radiotracers is fraught with pitfalls due to the amplifying effects of small quantities of radioactive impurities. For example, a radiotracer with a log P of 4 containing only 0.1% of a radioactive impurity with a log P of -1 will have an apparent log P of 3 if measured using conventional shake-flask partition techniques, counting the radioactivity in each phase. However, pre-washing the radiotracer-containing organic phase with aqueous phase can, in many cases, allay doubts about the validity of such measurements.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Octanol
  • Animals
  • Chemical Phenomena
  • Chemistry, Physical
  • Drug Contamination
  • Humans
  • Lipids / chemistry
  • Quantitative Structure-Activity Relationship
  • Radioisotopes / chemistry*
  • Radioisotopes / isolation & purification
  • Scintillation Counting
  • Solvents
  • Water

Substances

  • Lipids
  • Radioisotopes
  • Solvents
  • Water
  • 1-Octanol