Automated radiochemical synthesis and biodistribution of [¹¹C]l-α-acetylmethadol ([¹¹C]LAAM)

Appl Radiat Isot. 2014 Sep:91:135-40. doi: 10.1016/j.apradiso.2014.05.019. Epub 2014 Jun 2.

Abstract

Long-acting opioid agonists methadone and l-α-acetylmethadol (LAAM) prevent withdrawal in opioid-dependent persons. Attempts to synthesize [(11)C]-methadone for PET evaluation of brain disposition were unsuccessful. Owing, however, to structural and pharmacologic similarities, we aimed to develop [(11)C]LAAM as a PET ligand to probe the brain exposure of long-lasting opioids in humans. This manuscript describes [(11)C]LAAM synthesis and its biodistribution in mice. The radiochemical synthetic strategy afforded high radiochemical yield, purity and specific activity, thereby making the synthesis adaptable to automated modules.

Keywords: Biodistribution; LAAM; Methadone; PET; Positron emission tomography; l-α-Acetylmethadol.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Brain / metabolism
  • Carbon Radioisotopes / chemistry*
  • Male
  • Methadyl Acetate / chemical synthesis*
  • Methadyl Acetate / pharmacokinetics*
  • Mice
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics*
  • Tissue Distribution

Substances

  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Methadyl Acetate