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

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

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  • 1Department of Radiology, Washington University in St. Louis, St. Louis, MO 63110, USA; Department of Radiology, Wake Forest School of Medicine, 1 Medical Center Blvd, Winston Salem, NC 27157, USA.
  • 2Department of Radiology, Washington University in St. Louis, St. Louis, MO 63110, USA; Department of Radiology, University of Alabama School of Medicine, 720 2nd Ave S, Birmingham, AL 35294, USA.
  • 3Department of Radiology, Washington University in St. Louis, St. Louis, MO 63110, USA.
  • 4Department of Radiology, Washington University in St. Louis, St. Louis, MO 63110, USA; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, 231 S. 34th Street, Philadelphia, PA 19104, USA.
  • 5Department of Anesthesiology, and Department of Biochemistry and Molecular Biophysics, Washington University in St. Louis, 660 S. Euclid Ave., Campus Box 8054, St. Louis, MO 63110, USA. Electronic address: kharasch@wustl.edu.

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.

Copyright © 2014. Published by Elsevier Ltd.

KEYWORDS:

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

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