2011
DOI: 10.1016/j.bmc.2011.10.028
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Abstract: The synthesis and structure-activity relationships of 8-substituted-3-[2-(diarylmethoxyethylidenyl)]-8-azabicyclo[3.2.1]octane derivatives were investigated at the dopamine transporter(DAT), the serotonin transporter (SERT) and norepinephrine transporter (NET). The rigid ethylidenyl-8-azabicyclic[3.2.1]octane skeleton imparted modestly stereoselective binding and uptake inhibition at the DAT. Additional structure-activity studies provided a transporter affinity profile that was reminiscent of the structure-act… Show more

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Cited by 2 publications
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“…18 The monoamine transporter binding affinities of the 3-arylmethoxy-3-aryl-azetidines ( 6 ) were generally selective for the SERT over the DAT exhibiting nanomolar affinity for the SERT and micromolar affinity for the DAT. The dichloro substituted congeners 6e ( K i = 3.5 nM) and 6h ( K i = 2.9 nM) were the most potent of the azetidines at SERT.…”
mentioning
confidence: 99%
“…18 The monoamine transporter binding affinities of the 3-arylmethoxy-3-aryl-azetidines ( 6 ) were generally selective for the SERT over the DAT exhibiting nanomolar affinity for the SERT and micromolar affinity for the DAT. The dichloro substituted congeners 6e ( K i = 3.5 nM) and 6h ( K i = 2.9 nM) were the most potent of the azetidines at SERT.…”
mentioning
confidence: 99%