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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Sai, KKS; Fan, J; Tu, Z; Zerkel, P; Mach, RH; Kharasch, ED

Published Date

  • September 2014

Published In

Volume / Issue

  • 91 /

Start / End Page

  • 135 - 140

PubMed ID

  • 24935116

Pubmed Central ID

  • PMC4384447

Electronic International Standard Serial Number (EISSN)

  • 1872-9800

Digital Object Identifier (DOI)

  • 10.1016/j.apradiso.2014.05.019


  • eng

Conference Location

  • England