Lemaire C, Cantineau R, Guillaume M, Plenevaux A, Christiaens L
Cyclotron Research Center, Liège University, Belgium.
J Nucl Med. 1991 Dec;32(12):2266-72.
No-carrier-added [18F]altanserin was synthesized by nucleophilic substitution of the corresponding nitro compound with [18F]fluoride in the presence of kryptofix 222 and K2CO3. After purification by preparative HPLC, [18F]altanserin was produced in less than 2 hr with a radiochemical yield of 10% (EOS) and a specific activity of 0.8-1.3 Ci/mumol. In rats, the tracer localized rapidly in the whole brain (0.5% ID/g organ) with a high binding to the frontal cortex. The frontal cortex/cerebellum ratio increased with time and reached a plateau of 11 at 2 hr postinjection. This uptake in S2 receptor regions was saturable and could be blocked by pretreatment with various S2 antagonists. This radiopharmaceutical appears to be more selective for S2 receptor sites than other ligands available today and allows the study of S2 receptors under in vivo conditions.
无载体添加的[18F]阿坦色林通过在穴状配体222和碳酸钾存在下，用[18F]氟化物对相应的硝基化合物进行亲核取代反应合成。经制备型高效液相色谱法纯化后，[18F]阿坦色林在不到2小时内制备完成，放射化学产率为10%（放化纯），比活度为0.8 - 1.3 Ci/μmol。在大鼠中，该示踪剂迅速在全脑定位（0.5%注射剂量/克组织），并与额叶皮质有高度结合。额叶皮质/小脑的比值随时间增加，在注射后2小时达到11的平台期。在S2受体区域的摄取是可饱和的，并且可以被各种S2拮抗剂预处理所阻断。这种放射性药物似乎比目前可用的其他配体对S2受体位点更具选择性，并且能够在体内条件下对S2受体进行研究。
