Document Detail


Effect of 2-(4-aminophenylmethyl)-6-hydroxy-3, 4-dihydronaphthalen-1(2H)-one on all-trans and 13-cis-retinoic acid levels in plasma quantified by high perfomance liquid chromatography coupled to tandem mass spectrometry.
MedLine Citation:
PMID:  16119191     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The effect of the titled tetralone as a retinoic acid metabolism blocking agent (RAMBA) in vivo in comparison with ketoconazole, a well known cytochrome P450 inhibitor, was studied. Development of a HPLC/MS/MS method for the quantification of retinoic acid levels extracted from rat plasma was used to demonstrate that ketoconazole and the tetralone (100 mg/kg) enhanced the endogenous plasma concentration of retinoic acid. Levels of retinoid were raised from a control value of 0.11 to 0.15 and 0.17 ng/mL after treatment with tetralone and ketoconazole respectively showing that the tetralone and ketoconazole lead to comparable effects, indicating an inhibitory activity of the tetralone on retinoic acid metabolism.
Authors:
Marc Angotti; Rolf W Hartmann; Andrew J Kirby; Claire Simons; Paul J Nicholls; Robert D E Sewell; H John Smith
Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Journal of enzyme inhibition and medicinal chemistry     Volume:  20     ISSN:  1475-6366     ISO Abbreviation:  J Enzyme Inhib Med Chem     Publication Date:  2005 Jun 
Date Detail:
Created Date:  2005-08-25     Completed Date:  2005-12-02     Revised Date:  2007-03-21    
Medline Journal Info:
Nlm Unique ID:  101150203     Medline TA:  J Enzyme Inhib Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  219-26     Citation Subset:  IM    
Affiliation:
Pharmaceutical and Medicinal Chemistry, Saarland University, Universität des Saarlandes, PO Box 15 11 50, D-66041 Saarbrücken, Germany. rwh@mx.uni-saarland.de
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MeSH Terms
Descriptor/Qualifier:
Animals
Chromatography, High Pressure Liquid / methods*
Isotretinoin / blood*,  chemistry
Ketoconazole / metabolism,  pharmacology
Male
Mass Spectrometry
Naphthalenes / pharmacology*
Rats
Rats, Inbred WF
Spectrometry, Mass, Electrospray Ionization / methods*
Tetralones / metabolism,  pharmacology
Tretinoin / blood*,  chemistry
Chemical
Reg. No./Substance:
0/2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one; 0/Naphthalenes; 0/Tetralones; 302-79-4/Tretinoin; 4759-48-2/Isotretinoin; 65277-42-1/Ketoconazole

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


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