Abstract
Herein we report the synthesis of a series of bicyclo[3.2.1]octanes and their binding characteristics at the dopamine and serotonin transporters. The data confirm that a heteroatom at position 8 of the tropane nucleus is not a prerequisite for binding since the bicyclo[3.2.1]octanes prove potent inhibitors of both transporters. Therefore the three-dimensional topology of the ligand may be more important than specific functionality with respect to stereospecific binding at the acceptor site.
Publication types
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Comparative Study
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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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Carrier Proteins / metabolism*
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Cocaine / chemistry
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Dopamine Plasma Membrane Transport Proteins
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Inhibitory Concentration 50
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Kinetics
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Membrane Glycoproteins / metabolism*
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Membrane Transport Proteins*
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Models, Chemical
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Nerve Tissue Proteins*
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Serotonin Plasma Membrane Transport Proteins
Substances
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Bridged Bicyclo Compounds
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Serotonin Plasma Membrane Transport Proteins
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Cocaine