Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter.
Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter.
复制标题
一系列新型托烷 N- 或 O- 氟烷基衍生物的合成和生物学评价：用于多巴胺转运蛋白的潜在正电子发射断层扫描 (PET) 成像剂。
DOI：
10.1016/s0960-894x(01)00626-6
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发表时间：
2001
影响因子：
2.7
通讯作者：
Neumeyer,JL
中科院分区：
文献类型：
--
作者：
Gu,XH;Zong,R;Kula,NS;Baldessarini,RJ;Neumeyer,JL
A series of novel fluoroalkyl-containing tropane derivatives was synthesized, and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) were determined via competitive binding assays. Among these derivatives, the fluoropropyl ester of β-CIT (19), the fluoroethyl ester of β-CIT (20), the N-fluoropropyl derivative of β-CBT (12), and the fluoropropyl ester of β-CMT (18) displayed higher affinity and greater selectivity for the DAT versus SERT and NET than FP-CIT, which indicates that they are attractive candidates for the development of18F-labeled PET imaging agents for the DAT.
