Document Detail

Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
MedLine Citation:
PMID:  3031294     Owner:  NLM     Status:  MEDLINE    
Baclofen (beta-p-chlorophenyl-GABA) is the only selective agonist for the bicuculline-insensitive GABAB receptor. We report the synthesis of new GABA analogues and baclofen analogues. In vitro, two compounds, 4-amino-3-benzo[b]furan-2-ylbutanoic acid (9g) and 4-amino-3-(5-methoxybenzo[b]furan-2-yl)butanoic acid (9h), showed an affinity for the GABAB receptor. The results obtained with racemic compounds of benzofuran structure, new for this series, and the surprising inactivity of compound 3a (4-amino-3-(4-hydroxyphenyl)butanoic acid) permit the proposal of an hypothesis for the structure-activity relationships with regard to GABAB receptor.
P Berthelot; C Vaccher; A Musadad; N Flouquet; M Debaert; M Luyckx
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  30     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1987 Apr 
Date Detail:
Created Date:  1987-05-11     Completed Date:  1987-05-11     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  743-6     Citation Subset:  IM    
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MeSH Terms
Baclofen / analogs & derivatives*,  chemical synthesis,  metabolism,  pharmacology
Cerebral Cortex / metabolism
Rats, Inbred Strains
Receptors, GABA-A / drug effects*,  metabolism
Receptors, GABA-B
Structure-Activity Relationship
gamma-Aminobutyric Acid / analogs & derivatives*,  chemical synthesis,  metabolism,  pharmacology
Reg. No./Substance:
0/Receptors, GABA-A; 0/Receptors, GABA-B; 1134-47-0/Baclofen; 56-12-2/gamma-Aminobutyric Acid

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

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