Synthesis and monoamine transporter binding properties of 3 alpha-(substituted phenyl)nortropane-2 beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds

3 alpha-(Substituted phenyl)nortropane-2 beta-carboxylic acid methyl esters (8a-h) showed high affinity for the norepinephrine transporter (NET). The most potent and selective compound was 3 alpha-(3-fluoro-4-methylphenyl)nortropane-2 beta-carboxylic acid methyl ester (8d), with a K-i of 0.43 nM at the NET and 21- and 55-fold selectivity relative to binding at the dopamine and serotonin transporters. The development of 8d makes available compounds selective for all three transporters from the same structural class

Carroll, F., Tyagi, S., Blough, B., Kuhar, MJ., & Navarro, H. (2005). Synthesis and monoamine transporter binding properties of 3 alpha-(substituted phenyl)nortropane-2 beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. Journal of Medicinal Chemistry, 48(11), 3852-3857.