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

Autor: Stehouwer, J. S., Plisson, C., Jarkas, N., Zeng, F., Voll, R. J., Williams, L., Martarello, L., Votaw, J. R., Tamagnan, G., Goodman, M. M.
Zdroj: Journal of Medicinal Chemistry; November 2005, Vol. 48 Issue: 22 p7080-7083, 4p
Abstrakt: 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.
Databáze: Supplemental Index