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 pr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2003-11, Vol.11 (23), p.4949-4958
Hauptverfasser:	BYOUNG SE LEE, SOYOUNG CHU, KYO CHUL LEE, LEE, Bon-Su, DAE YOON CHI, YEARN SEONG CHOE, SANG EUN KIM, YUN SEON SONG, CHANGBAE JIN
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Carrier Proteins - chemical synthesis Carrier Proteins - metabolism Chromatography, High Pressure Liquid Contrast media. Radiopharmaceuticals Magnetic Resonance Spectroscopy Medical sciences Membrane Glycoproteins - chemical synthesis Membrane Glycoproteins - metabolism Membrane Transport Proteins Mice Nerve Tissue Proteins - chemical synthesis Nerve Tissue Proteins - metabolism Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Quipazine - analogs & derivatives Quipazine - chemical synthesis Quipazine - metabolism Serotonin Plasma Membrane Transport Proteins Serotoninergic system Spectrometry, Mass, Electrospray Ionization Spectrometry, Mass, Fast Atom Bombardment Tissue Distribution
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Zusammenfassung:	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.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2003.09.009