Document Detail

Investigation into the in vivo effects of five novel tacrine/ferulic acid and beta-carboline derivatives on scopolamine-induced cognitive impairment in rats using radial maze paradigm.
MedLine Citation:
PMID:  20648918     Owner:  NLM     Status:  MEDLINE    
Two tacrine-ferulic acid hybrids (1 A, 1 B) and three beta-carboline derivatives (BCs; 2A, 2B, 2C) were tested in vivo on 3-month-old female rats as multi-potent anti-Alzheimer drug candidates. In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). However, in vivo both substances have no beneficial effect on scopolamine (CAS 51-34-3) induced cognition impairment. On the contrary, 1B even worsen the scopolamine induced cognition impairment. The beta-carboline derivatives 2A, 2B, and 2 C, the inhibitory potency of which at AChE reaching tacrine activity does not antagonize scopolamine induced impairment of cognition in rats measured in radial maze paradigm. Compounds 2A and 1B might act as positive allosteric modulators of scopolamine action at the muscarinic acetylcholine receptors. On the basis of these results it can be concluded that both ferulic acid- (CAS 537-98-4) and BC-derivatives are not qualified as cognition improving drugs and further studies in this field should be focussed on other pharmaceutical leads to find effective anti-Alzheimer drugs.
Christian Fleck; Dorothea Appenroth; Lei Fang; Yvonne Schott; Jochen Lehmann; Michael Decker
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  60     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  2010  
Date Detail:
Created Date:  2010-07-22     Completed Date:  2010-09-21     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  299-306     Citation Subset:  IM    
Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany.
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MeSH Terms
Carbolines / pharmacology*
Cognition / drug effects*
Cognition Disorders / chemically induced*,  psychology
Coumaric Acids / pharmacology*
Maze Learning / drug effects*
Rats, Wistar
Receptors, Cholinergic / drug effects,  physiology
Receptors, Muscarinic / drug effects,  physiology
Scopolamine / pharmacology*
Tacrine / pharmacology*
Reg. No./Substance:
0/Carbolines; 0/Coumaric Acids; 0/Receptors, Cholinergic; 0/Receptors, Muscarinic; 1135-24-6/ferulic acid; 321-64-2/Tacrine; 51-34-3/Scopolamine

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