651315-44-5Relevant articles and documents
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter: Part 3. A potential 5-HT transporter imaging agent, 3-(3-[18F]Fluoropropyl)-6-nitroquipazine
Lee, Byoung Se,Chu, Soyoung,Lee, Kyo Chul,Lee, Bon-Su,Chi, Dae Yoon,Choe, Yearn Seong,Kim, Sang Eun,Song, Yun Seon,Jin, Changbae
, p. 4949 - 4958 (2003)
3-(3-[18F]Fluoropropyl)-6-nitroquipazine ([18F]FPNQ) as a 5-HT transporter imaging agents was designed, synthesized, and evaluated. FPNQ was selected due to its potent in vitro biological activity (K i=0.32 nM) in rat brain cortical membranes. The 18F- labeled FPNQ was prepared by reaction of the propyl mesylate as a precursor with tetra-n-butylammonium [18F]fluoride generated under NCA conditions. The precursor mesylate was synthesized from commercially available hydrocarbostyril in nine steps in 21% overall yield. The specific activity of the [18F]FPNQ determined by radioreceptor assay was 27.0 GBq/μmol. Tissue distribution studies in mice showed the highest uptake in the frontal cortex (5.79%ID/g) at 60 min post-injection.