Hocke Carsten, Prante Olaf, Löber Stefan, Hübner Harald, Gmeiner Peter, Kuwert Torsten
Department of Nuclear Medicine, Krankenhausstrasse 12, D-91054 Erlangen, Germany.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3963-6. doi: 10.1016/j.bmcl.2004.05.052.
Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding data showed a 15-560-fold selectivity for the dopamine D3 over D2. A 2,3-dichloro substitution pattern on the phenylpiperazine moiety led to the highest subtype selectivity, whereas the 2-methoxy substituted compounds showed superior D3 affinity. Suitable precursors were radioiodinated with high radiochemical yields (53-85%) leading to potential imaging agents for the D3 receptor by SPET.
从FAUC 365开始，已经合成了一系列碘取代的杂芳基羧酰胺，这些化合物对多巴胺D3受体显示出高亲和力和选择性。结合数据表明，多巴胺D3相对于D2的选择性为15至560倍。苯基哌嗪部分上的2,3-二氯取代模式导致了最高的亚型选择性，而2-甲氧基取代的化合物显示出优异的D3亲和力。合适的前体以高放射化学产率（53-85%）进行放射性碘化，通过单光子发射断层扫描（SPET）产生了用于D3受体的潜在成像剂。
