Lee, BS Chu, S Lee, KC Lee, BS Chi, DY Choe, YS Kirn, SE Song, YS Jin, C 2024-01-21T08:03:04Z 2024-01-21T08:03:04Z 2021-09-03 2003-11-17 0968-0896 https://pubs.kist.re.kr/handle/201004/138081 3-(3-[F-18]Fluoropropyl)-6-nitroquipazine ([F-18]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 F-18-labeled FPNQ was prepared by reaction of the propyl mesylate as a precursor with tetra-n-butylammonium [F-18]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 [F-18]FPNQ determined by radioreceptor assay was 27.0 GBq/mumol. Tissue distribution studies in mice showed the highest uptake in the frontal cortex (5.79 %ID/g) at 60 min post-injection. (C) 2003 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD POSITRON-EMISSION-TOMOGRAPHY 5-HYDROXYTRYPTAMINE UPTAKE COMPLEX DOPAMINE TRANSPORTER H-3 6-NITROQUIPAZINE IN-VIVO I-125 5-IODO-6-NITROQUIPAZINE PARKINSONS-DISEASE SELECTIVE LIGAND UPTAKE SITES RAT-BRAIN Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter: Part 3. A potential 5-HT transporter imaging agent, 3-(3-[F-18]fluoropropyl)-6-nitroquipazine Article 10.1016/j.bmc.2003.09.009 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.11, no.23, pp.4949 - 4958 BIOORGANIC & MEDICINAL CHEMISTRY 11 23 4949 4958 scie scopus 000186614400011 2-s2.0-0242298240 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article POSITRON-EMISSION-TOMOGRAPHY 5-HYDROXYTRYPTAMINE UPTAKE COMPLEX DOPAMINE TRANSPORTER H-3 6-NITROQUIPAZINE IN-VIVO I-125 5-IODO-6-NITROQUIPAZINE PARKINSONS-DISEASE SELECTIVE LIGAND UPTAKE SITES RAT-BRAIN serotonin transporter 6-nitroquipazine analogues binding affinities imaging agent 3-(3-[18F]fluoropropyl)-6-nitroquipazine