Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 15, Pages 3427-3430Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070131b
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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.
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