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 |
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Authors: | Angotti Marc Hartmann Rolf W Kirby Andrew J Simons Claire Nicholls Paul J Sewell Robert D E Smith H John |
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Institution: | Pharmaceutical and Medicinal Chemistry, Saarland University, Universit?t des Saarlandes, PO Box 15 11 50, D-66041 Saarbrücken, Germany. rwh@mx.uni-saarland.de |
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Abstract: | 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. |
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