| Literature DB >> 17608398 |
Ping Liu, Linus S Lin, Terence G Hamill, James P Jewell, Thomas J Lanza, Raymond E Gibson, Stephen M Krause, Christine Ryan, Waisi Eng, Sandra Sanabria, Xinchun Tong, Junying Wang, Dorothy A Levorse, Karen A Owens, Tung M Fong, Chun-Pyn Shen, Julie Lao, Sanjeev Kumar, Wenji Yin, Joseph F Payack, Shawn A Springfield, Richard Hargreaves, H Donald Burns, Mark T Goulet, William K Hagmann.
Abstract
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 18F to the molecule was developed. Further optimization focused on reducing the lipophilicity and increasing the CB1R affinity. These efforts led to the identification of [18F]-16 that exhibited good brain uptake and an excellent signal-to-noise ratio in rhesus monkeys.Entities:
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Year: 2007 PMID： 17608398 DOI： 10.1021/jm070131b
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446