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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. Copyright © 2014. Published by Elsevier Ltd.

Citation

Kiran Kumar Solingapuram Sai, Jinda Fan, Zhude Tu, Patrick Zerkel, Robert H Mach, Evan D Kharasch. Automated radiochemical synthesis and biodistribution of [¹¹C]l-α-acetylmethadol ([¹¹C]LAAM). Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine. 2014 Sep;91:135-40

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PMID: 24935116

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