Abstract
A series of 16 new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropane derivatives was synthesized and evaluated for binding to monoamine transporters. Most of the compounds exhibited nanomolar affinity for the serotonin transporter (SERT). Four compounds presented a particularly attractive pharmacological profile, with very high SERT affinity (K(i) 0.15-0.5 nM) and selectivity versus the dopamine transporter of 25- to 77-fold.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Cell Membrane / metabolism
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Chemistry, Pharmaceutical / methods
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Cocaine / analogs & derivatives*
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Cocaine / chemical synthesis
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Cocaine / chemistry
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Dopamine Plasma Membrane Transport Proteins / chemistry
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Drug Design
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Humans
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Kinetics
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Models, Chemical
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Prosencephalon / metabolism
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Protein Binding
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Protein Transport
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Rats
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Serotonin Plasma Membrane Transport Proteins / chemistry
Substances
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Dopamine Plasma Membrane Transport Proteins
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Serotonin Plasma Membrane Transport Proteins
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troparil
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Cocaine