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合成了用作外周苯二氮受体潜在的选择性配体的N,N-二乙基-2-(4-碘苯基)-6-三氟甲基-咪唑并[1,2-a]吡啶-3-乙酰胺(ITFZOL).其放射性标记物[125I]ITFZOL通过碘脱锡化反应制备,放化得率75%~85%,比活度大于76GBq/μmol.小鼠尾静脉注射[125I]ITFZIOL后,放射性集中分布于肾上腺、肺、肾、心、嗅球和小脑等外周苯二氮受体高密度区域.预先给与外周苯二氮受体选择性配体PK11195明显减少外周苯二氮受体高密度区域放射性分布,提示[125I]ITFZOL对外周苯二氮受体具有较高的特异亲和性.生物活性数据表明,[125I]ITFZO是一种潜在的选择性外周苯二氮受体单光子放射性配体.
Synthesis of N, N-diethyl-2- (4-iodophenyl) -6-trifluoromethyl-imidazo [1,2- a] pyridine-3-acetamide (ITFZOL) .Its radioactive label [125I] ITFZOL was prepared by iodination-decylation and its radiochemical yield was 75% -85% and its specific activity was more than 76GBq / After injection of [125I] ITFZIOL, the radioactivity was concentrated in the peripheral high-density region of benzodiazepine receptors such as adrenal, lung, kidney, heart, olfactory bulb and cerebellum.Peral administration of benzodiazepine ligand selective ligand PK11195 Reduce the distribution of peripheral benzodiazepine receptor high-density region, suggesting that [125I] ITFZOL has a higher specific affinity for peripheral benzodiazepine receptors. Bioactivity data show that [125I] ITFZO is a potential Selective peripheral benzodiazepine receptor single photon radioligand.