Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Fluorine-18 (N-Fluoroalkyl) Labeled 2β-Carbomethoxy-3β-(4'-(3-furyl)phenyl)tropanes and -nortropanes:  Candidate Radioligands for in Vivo Imaging of the Serotonin Transporter with Positron Emission Tomography

2β-Carbomethoxy-3β-(4‘-(3-furyl)phenyl)nortropane (1) was synthesized along with the N-methyl (2), N-fluoroethyl (3), N-fluoropropyl (4), and N-fluorobutyl (5) derivatives. The binding affinity for each compound to the human serotonin, dopamine, and norepinephrine transporters was determined using t...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2005-11, Vol.48 (22), p.7080-7083
Main Authors: Stehouwer, Jeffrey S, Plisson, Christophe, Jarkas, Nachwa, Zeng, Fanxing, Voll, Ronald J, Williams, Larry, Martarello, Laurent, Votaw, John R, Tamagnan, Gilles, Goodman, Mark M
Format: Article
Language:English
Subjects:
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Medical sciences
Pharmacology. Drug treatments
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Summary:2β-Carbomethoxy-3β-(4‘-(3-furyl)phenyl)nortropane (1) was synthesized along with the N-methyl (2), N-fluoroethyl (3), N-fluoropropyl (4), and N-fluorobutyl (5) derivatives. The binding affinity for each compound to the human serotonin, dopamine, and norepinephrine transporters was determined using transfected HEK-293 cells. Radiolabeling and microPET brain imaging studies were performed with [11C]1, [11C]2, and [18F]3 to determine their utility as in vivo imaging agents.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0504095