Discovery of N-{(1S,2S)-2-(3-Cyanophenyl)-3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}-2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use
Discovery of N-{(1S,2S)-2-(3-Cyanophenyl)-3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}-2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use
复制标题
DOI：
10.1021/jm070131b
复制
发表时间：
2007-07-26
影响因子：
7.3
通讯作者：
Hagmann, William K.
中科院分区：
文献类型：
--
作者：
Liu, Ping;Lin, Linus S.;Hagmann, William K.
描述了一种结构上不同的大麻素-1受体（CB 1 R）正电子发射断层扫描示踪剂的发现。以无环酰胺CB 1 R反向激动剂（1）为先导化合物，开发了一种将F-18引入分子的有效途径。进一步的优化集中在降低亲脂性和增加CB 1 R亲和力。这些努力导致鉴定出[F-18]-16在恒河猴中表现出良好的脑摄取和优异的信噪比。
The discovery of a structurally distinct cannabinoid-1 receptor (CB1R) positron emission tomography tracer is described. Starting from an acyclic amide CB1R inverse agonist (1) as the lead compound, an efficient route to introduce F-18 to the molecule was developed. Further optimization focused on reducing the lipophilicity and increasing the CB1R affinity. These efforts led to the identification of [F-18]-16 that exhibited good brain uptake and an excellent signal-to-noise ratio in rhesus monkeys.