Document Detail

Synthesis and monoamine uptake inhibition of conformationally constrained 2beta-carbomethoxy-3beta-phenyl tropanes.
MedLine Citation:
PMID:  19532984     Owner:  NLM     Status:  MEDLINE    
A series of 2beta-carbomethoxy-3beta-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity.
Patrick Johannes Riss; René Hummerich; Patrick Schloss
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-04-29
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  7     ISSN:  1477-0539     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-17     Completed Date:  2009-09-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  2688-98     Citation Subset:  IM    
Institute of Nuclear Chemistry, Johannes Gutenberg-University Mainz, Fritz Strassmann-Weg 2, 55128, Mainz, Germany.
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MeSH Terms
Biogenic Monoamines / antagonists & inhibitors,  metabolism*
Biological Transport / drug effects
Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors*
Molecular Conformation
Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors
Serotonin Plasma Membrane Transport Proteins / drug effects
Structure-Activity Relationship
Tropanes / chemical synthesis*,  chemistry,  pharmacology*
Reg. No./Substance:
0/Biogenic Monoamines; 0/Dopamine Plasma Membrane Transport Proteins; 0/Ligands; 0/Norepinephrine Plasma Membrane Transport Proteins; 0/Serotonin Plasma Membrane Transport Proteins; 0/Tropanes

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