Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
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作为潜在正电子发射断层扫描（PET）成像剂的新型苯托烷衍生物的合成和胺转运蛋白亲和力。
DOI：
10.1016/j.bmcl.2004.08.049
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
Neumeyer,JohnL
中科院分区：
文献类型：
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作者：
Peng,Xuemei;Zhang,Ao;Kula,NoraS;Baldessarini,RossJ;Neumeyer,JohnL
A series of novel fluoroalkyl-containing tropane derivatives (6–8, 10–14, 17, and 18) were synthesized from cocaine. Novel compounds were evaluated for affinity and selectivity in competitive radioligand binding assays selective for cerebral serotonin (5-HT), dopamine (DA), and norepinephrine (NE) transporters (SERT, DAT, and NET). The nortropane-fluoroalkyl esters (7, 10, 11) were most potent for SERT (Ki: 0.18, 0.24, and 0.30nM, respectively). Tosylate esters 17 and 18, synthesized as precursors for [18F]-labeled, Positron Emission Tomography (PET) imaging agents, also showed high affinity for DAT.
