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

Kiran Kumar Solingapuram Sai, Jinda Fan, Zhude Tu, Patric Zerkel, Robert H. Mach, Evan D. Kharasch

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Long-acting opioid agonists methadone and l-α-acetylmethadol (LAAM) prevent withdrawal in opioid-dependent persons. Attempts to synthesize [11C]-methadone for PET evaluation of brain disposition were unsuccessful. Owing, however, to structural and pharmacologic similarities, we aimed to develop [11C]LAAM as a PET ligand to probe the brain exposure of long-lasting opioids in humans. This manuscript describes [11C]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.

Original languageEnglish
Pages (from-to)135-140
Number of pages6
JournalApplied Radiation and Isotopes
Volume91
DOIs
StatePublished - Sep 2014

Keywords

  • Biodistribution
  • L-α-Acetylmethadol
  • LAAM
  • Methadone
  • PET
  • Positron emission tomography

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