Document Detail

Synthesis and biological evaluation of a technetium-99m(I)-tricarbonyl-labelled phenyltropane derivative.
MedLine Citation:
PMID:  16271471     Owner:  NLM     Status:  MEDLINE    
A new tropane derivative was synthesized by combining a tridentate ligand, N-(2-picolylamine)-N-acetic acid (2-PAA), and a phenyltropane derivative. It was labelled with a [(99m)Tc(CO)(3)](+) moiety, resulting in the formation of two stable and neutral lipophilic isomers. Their identity was confirmed using radio-LC-MS. In normal mice, no brain uptake was observed for any of the isomers and in vitro autoradiography using mouse brain sections showed no specific uptake in the striatal area.
Davy M Kieffer; Bernard J Cleynhens; Hubert P Vanbilloen; Dirk Rattat; Christelle Y Terwinghe; Luc Mortelmans; Guy M Bormans; Alfons M Verbruggen
Publication Detail:
Type:  In Vitro; Journal Article     Date:  2005-11-03
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Jan 
Date Detail:
Created Date:  2005-11-25     Completed Date:  2006-03-02     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  382-6     Citation Subset:  IM    
Laboratory of Radiopharmaceutical Chemistry, University Hospital Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.
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MeSH Terms
Brain / drug effects,  metabolism
Drug Evaluation, Preclinical
Isotope Labeling
Molecular Conformation
Organotechnetium Compounds / chemistry*
Structure-Activity Relationship
Tissue Distribution
Tropanes / chemical synthesis*,  chemistry,  pharmacokinetics*
Reg. No./Substance:
0/Organotechnetium Compounds; 0/Tropanes

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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