[18F]N-(2-(二乙氨基)乙基)-6-氟烟酰胺的发现：一种用于黑色素瘤正电子发射断层显像的放射性示踪剂，具有高肿瘤与机体对比率及快速肾脏清除率。
Discovery of [18F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide: a melanoma positron emission tomography imaging radiotracer with high tumor to body contrast ratio and rapid renal clearance.
作者信息
Greguric Ivan, Taylor Stephen R, Denoyer Delphine, Ballantyne Patrice, Berghofer Paula, Roselt Peter, Pham Tien Q, Mattner Filomena, Bourdier Thomas, Neels Oliver C, Dorow Donna S, Loc'h Christian, Hicks Rodney J, Katsifis Andrew
机构信息
Radiopharmaceuticals Research Institute, Australian Nuclear Science and Technology Organisation, Menai, NSW 2234, Sydney, Australia.
出版信息
J Med Chem. 2009 Sep 10;52(17):5299-302. doi: 10.1021/jm9008423.
The high melanoma uptake and rapid body clearance displayed by our series of [(123)I]iodonicotinamides prompted the development of [(18)F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([(18)F]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [(18)F]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [(18)F]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.
我们的一系列[(123)I]碘烟酰胺显示出高黑色素瘤摄取率和快速的体内清除率，促使研发出[(18)F]N-(2-(二乙氨基)乙基)-6-氟烟酰胺([(18)F]2)，一种用于PET黑色素瘤成像的新型放射性示踪剂。值得注意的是，与氟苯甲酸酯不同，[(18)F]氟在烟酰胺环上的掺入是一步完成的，操作简便且产率高。[(18)F]2显示出高肿瘤摄取率，主要通过肾脏排泄实现快速的体内清除，目前正在进行临床前研究评估，以推进到临床试验阶段，用于评估治疗药物的反应性。
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