Abstract
A series of 3-{2-(diarylmethoxyethylidene)}-8-alkylaryl-8-azabicyclo[3.2.1]octanes was synthesized and the binding affinities of the compounds were determined at the dopamine and serotonin transporters. The 8-phenylpropyl analogues
8a (
K
i=4.1
nM) and
8b (
K
i=3.7
nM) were the most potent compounds of the series with binding affinities 3 times greater than GBR-12909. In addition,
8a (SERT/DAT=327) was over 300-fold more selective for the dopamine transporter than the serotonin transporter.
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