Abstract
A series of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes was synthesized and the binding affinities of the compounds were determined at the dopamine transporter. The unsubstituted analogue 7b (K(i)=98nM) was the most potent compound of the series with binding affinity three-times greater than cocaine and only 5-fold less than GBR-12909. The structure-activity data for 7a-f suggests that these compounds may be binding at the dopamine transporter in a similar fashion to GBR 12909.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / pharmacology
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors / chemical synthesis*
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Dopamine Uptake Inhibitors / pharmacology
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Humans
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Membrane Glycoproteins*
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Membrane Transport Modulators
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Membrane Transport Proteins / antagonists & inhibitors
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Membrane Transport Proteins / metabolism*
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Nerve Tissue Proteins*
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Octanes / chemical synthesis
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Octanes / pharmacology
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Protein Binding
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Structure-Activity Relationship
Substances
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Bridged Bicyclo Compounds
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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Membrane Glycoproteins
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Membrane Transport Modulators
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Octanes