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.
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/micromol. Tissue distribution studies in mice showed the highest uptake in the frontal cortex (5.79 %ID/g) at 60 min post-injection.
Lee
Byoung Se
BS
Department of Chemistry, Inha University, 253 Yonghyundong Namgu, Inchon, 402-751, South Korea.
Chu
Soyoung
S
Lee
Kyo Chul
KC
Lee
Bon Su
BS
Chi
Dae Yoon
DY
Choe
Yearn Seong
YS
Kim
Sang Eun
SE
Song
Yun Seon
YS
Jin
Changbae
C
D000818:Animals; D002352:Carrier Proteins / Q000138:chemical synthesis* / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D009682:Magnetic Resonance Spectroscopy; D008562:Membrane Glycoproteins / Q000138:chemical synthesis* / Q000378:metabolism*; D026901:Membrane Transport Proteins; D051379:Mice; D009419:Nerve Tissue Proteins / Q000138:chemical synthesis* / Q000378:metabolism*; D011814:Quipazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000378:metabolism*; D050486:Serotonin Plasma Membrane Transport Proteins; D021241:Spectrometry, Mass, Electrospray Ionization; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014018:Tissue Distribution
D002352:Carrier Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D050486:Serotonin Plasma Membrane Transport Proteins; C493231:Slc6a4 protein, mouse; D011814:Quipazine; C031227:6-nitroquipazine