Document Detail


Enantiomerically Pure 1,3-Dioxanes as Highly Selective NMDA and σ1 Receptor Ligands.
MedLine Citation:
PMID:  23013229     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
We synthesized and investigated the NMDA and σ1 receptor affinity of enantiomerically pure 2 (2 phenyl-1,3 dioxan 4 yl)ethanamines 17 26. The primary amines (R,R) 18 20 with an axially oriented phenyl moiety in position 2 interacted with high enantioselectivity (eudismic ratios 70 130) and high affinity (Ki((R,R) 19) = 13 nM) with the PCP binding site of the NMDA receptor. Introduction of an N benzyl moiety led to potent σ1 ligands including compound (S,R) 22 (Ki = 6 nM) with an equatorially oriented phenyl moiety in position 2.
Authors:
Jens Köhler; Klaus Bergander; Jörg Fabian; Dirk Schepmann; Bernhard Wünsch
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-27
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-9-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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