Development of a high spec multivalent PET probe for molecular imaging of pain

在这里，我们证实了外周苯二氮卓类受体(PBR)作为激活的小胶质细胞的分子成像靶点的有效性，这是通过大鼠脑片中~3H标记的PBR配体的体外定量放射自显影显示的。设计了两种PBR配体偶联的GA-DOTA螯合物DOTA-PK2作为活化的小胶质细胞的多价PET探针。我们成功地合成了高放化纯度的~(67)Ga标记DOTA-MN_2。这些结果为用于疼痛分子成像的PET探针的化学设计提供了有用的信息。

Here we confirmed the validity of peripheral benzodiazepine receptors (PBR) as a target for molecular imaging of activated microglia, as revealed by quantitative in vitro autoradiography of ^3H-labeled PBR ligand in rat brain slices. A two PBR ligands-conjugated Ga-DOTA chelate, DOTA-PK2 was designed as a multivalent PET probe of activated microglia. We successfully synthesized a^67Ga-labeled DOTA-MN2 with high radiochemical purity. These results provide useful information about the chemical design of PET probe for molecular imaging of pain.