Sai Kiran Kumar Solingapuram, Fan Jinda, Tu Zhude, Zerkel Patrick, Mach Robert H, Kharasch Evan D
Department 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.
Department 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.
Appl Radiat Isot. 2014 Sep;91:135-40. doi: 10.1016/j.apradiso.2014.05.019. Epub 2014 Jun 2.
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.
长效阿片类激动剂美沙酮和左旋-α-乙酰美沙朵（LAAM）可防止阿片类药物依赖者出现戒断症状。曾尝试合成用于正电子发射断层扫描（PET）评估脑内分布的[(11)C]美沙酮，但未成功。然而，由于结构和药理学上的相似性，我们旨在开发[(11)C]LAAM作为PET配体，以探究长效阿片类药物在人体内的脑暴露情况。本手稿描述了[(11)C]LAAM的合成及其在小鼠体内的生物分布。放射化学合成策略提供了高放射化学产率、纯度和比活度，从而使该合成方法适用于自动化模块。
