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    
Abstract/OtherAbstract:
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.
Authors:
Christian Fleck; Dorothea Appenroth; Lei Fang; Yvonne Schott; Jochen Lehmann; Michael Decker
Related Documents :
2823318 - Nomenclature of lipoxins and related compounds derived from arachidonic acid and eicosa...
5661298 - Template-directed synthesis with adenosine-5'-phosphorimidazolide.
15333258 - Fsh isoform composition of commercial gonadotrophin preparations: a neglected aspect?
21821758 - Modification of the technical properties of lactobacillus johnsonii ncc 533 by suppleme...
15821508 - Physicochemical metabolic characteristics for calcium oxalate stone formation in patien...
2446838 - Purine receptors and kynurenic acid modulate the somatosensory evoked potential in rat ...
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    
Affiliation:
Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany. Christian.Fleck@mti.uni-jena.de
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Animals
Carbolines / pharmacology*
Cognition / drug effects*
Cognition Disorders / chemically induced*,  psychology
Coumaric Acids / pharmacology*
Female
Maze Learning / drug effects*
Rats
Rats, Wistar
Receptors, Cholinergic / drug effects,  physiology
Receptors, Muscarinic / drug effects,  physiology
Scopolamine / pharmacology*
Tacrine / pharmacology*
Chemical
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

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


Previous Document:  Influence of age on cognition and scopolamine induced memory impairment in rats measured in the radi...
Next Document:  Effect of lamotrigine and environmental enrichment on spatial memory and other behavioral functions ...