用于正电子发射断层显像（PET）成像研究的囊泡单胺摄取抑制剂[11C]丁苯那嗪的合成。

Synthesis of [11C]tetrabenazine, a vesicular monoamine uptake inhibitor, for PET imaging studies.

作者信息

DaSilva J N, Kilbourn M R, Mangner T J

机构信息

Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.

出版信息

Appl Radiat Isot. 1993 Apr;44(4):673-6. doi: 10.1016/0969-8043(93)90130-3.

DOI:10.1016/0969-8043(93)90130-3

PMID:8472029

Abstract

Tetrabenazine (TBZ), a high affinity and specific inhibitor of the vesicular monoamine transporter, has been labeled with carbon-11 as a potential probe for in vivo positron emission tomographic imaging of monoaminergic neuronal losses in neurodegenerative diseases. [11C]TBZ was synthesized by O-[11C]methylation of the 9-O-desmethylTBZ using [11C]methyl iodide in the presence of tetrabutylammonium hydroxide. The radiochemical yields were 35-55% (decay corrected) and the synthesis time 32-37 min from EOB. [11C]TBZ was obtained with specific activities of 2000-2500 Ci/mmol (EOS) and radiochemical and chemical purities were > 95%. [11C]Tetrabenazine is a promising new radioligand for the in vivo study of monoaminergic neurons using PET.

摘要

丁苯那嗪（TBZ）是一种对囊泡单胺转运体具有高亲和力的特异性抑制剂，已用碳-11标记，作为一种潜在的探针，用于在体正电子发射断层显像研究神经退行性疾病中单胺能神经元的损失。[11C]TBZ是在氢氧化四丁铵存在下，使用[11C]甲基碘对9-O-去甲基TBZ进行O-[11C]甲基化反应合成的。放射化学产率为35-55%（衰变校正），从EOB开始的合成时间为32-37分钟。[11C]TBZ的比活度为2000-2500 Ci/mmol（EOS），放射化学纯度和化学纯度均>95%。[11C]丁苯那嗪是一种有前景的新型放射性配体，可用于使用PET对单胺能神经元进行体内研究。