We successfully radiolabelled a novel prospective cannabinoid type 2 receptor ligand with ¹⁸F and tested its biodistribution in animal models by positron emission tomography (PET)/computed tomography (CT) imaging. The radiolabelling process was conducted on an alkyl mesylate fragment of the main naphthyridine core, using highly efficient microfluidic technology. No preliminary protection was needed, and the product was purified by semi-prep HPLC and SPE formulation, allowing the desired diastereomeric mixture to be obtained in 29 % radiochemical yield and > 95 % radiochemically pure. SOD1^G93A mice were used as model of overexpression of CB2 receptors; PET imaging revealed a significant increase of the tracer distribution volume in the brain of symptomatic subjects compared with the asymptomatic ones.

我们成功地用¹⁸ F放射性标记了新型前瞻性2型大麻素受体配体，并通过正电子发射断层扫描（PET）/计算机断层扫描（CT）成像测试了其在动物模型中的生物分布。使用高效的微流控技术对主要萘啶核的甲磺酸烷基酯片段进行了放射性标记。无需初步保护，产物通过半制备性HPLC和SPE制剂纯化，从而以29％的放射化学收率和> 95％的放射化学纯度获得所需的非对映异构混合物。SOD1 ^G93A小鼠用作CB2受体过表达的模型；PET成像显示，与无症状者相比，有症状受试者脑中示踪剂分布量显着增加。