Effect of α-Methyl versus α-Hydrogen Substitution on Brain Availability and Tumor Imaging Properties of Heptanoic [F-18]Fluoroalkyl Amino Acids for Positron Emission Tomography (PET)

J Med Chem. 2016 Apr 14;59(7):3515-31. doi: 10.1021/acs.jmedchem.6b00189. Epub 2016 Mar 23.

Abstract

Two [(18)F]fluoroalkyl substituted amino acids differing only by the presence or absence of a methyl group on the α-carbon, (S)-2-amino-7-[(18)F]fluoro-2-methylheptanoic acid ((S)-[(18)F]FAMHep, (S)-[(18)F]14) and (S)-2-amino-7-[(18)F]fluoroheptanoic acid ((S)-[(18)F]FAHep, (S)-[(18)F]15), were developed for brain tumor imaging and compared to the well-established system L amino acid tracer, O-(2-[(18)F]fluoroethyl)-l-tyrosine ([(18)F]FET), in the delayed brain tumor (DBT) mouse model of high-grade glioma. Cell uptake, biodistribution, and PET/CT imaging studies showed differences in amino acid transport of these tracer by DBT cells. Recognition of (S)-[(18)F]15 but not (S)-[(18)F]14 by system L amino acid transporters led to approximately 8-10-fold higher uptake of the α-hydrogen substituted analogue (S)-[(18)F]15 in normal brain. (S)-[(18)F]15 had imaging properties similar to those of (S)-[(18)F]FET in the DBT tumor model while (S)-[(18)F]14 afforded higher tumor to brain ratios due to much lower uptake by normal brain. These results have important implications for the future development of α-alkyl and α,α-dialkyl substituted amino acids for brain tumor imaging.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Substitution
  • Amino Acids / chemistry
  • Amino Acids / metabolism
  • Amino Acids / pharmacokinetics*
  • Amino Acids, Neutral / chemistry
  • Amino Acids, Neutral / metabolism
  • Amino Acids, Neutral / pharmacokinetics*
  • Animals
  • Biological Transport
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Brain Neoplasms / diagnostic imaging*
  • Brain Neoplasms / metabolism
  • Fluorine Radioisotopes / chemistry
  • Fluorine Radioisotopes / metabolism
  • Fluorine Radioisotopes / pharmacokinetics
  • Glioma / diagnostic imaging*
  • Glioma / metabolism
  • Hydrogen / chemistry*
  • Male
  • Methylation
  • Mice
  • Mice, Inbred BALB C
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacokinetics*
  • Tissue Distribution
  • Tyrosine / analogs & derivatives

Substances

  • 2-amino-7-fluoro-2-methylheptanoic acid
  • Amino Acids
  • Amino Acids, Neutral
  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Tyrosine
  • Hydrogen