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

作者:Sai Kiran Kumar Solingapuram; Fan Jinda; Tu Zhude; Zerkel Patrick; Mach Robert H; Kharasch Evan D*
来源:Applied Radiation and Isotopes, 2014, 91: 135-140.
DOI:10.1016/j.apradiso.2014.05.019

摘要

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

  • 出版日期2014-9