Journal
APPLIED RADIATION AND ISOTOPES
Volume 54, Issue 2, Pages 203-208Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0969-8043(00)00269-4
Keywords
lipophilicity; log P; QSAR; radiotracers
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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. (C) 2001 Elsevier Science Ltd. All rights reserved.
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