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RESEARCH PRODUCT
Retention-activity relationship studies of benzodiazepines by micellar liquid chromatography
M. Molero-monfortRosa María Villanueva-camañasM.j. Medina-hernándezSalvador Sagradosubject
PharmacologyChromatographyPassive transportChemistryMetaboliteClinical BiochemistryBiological membraneGeneral MedicineBiochemistryAnalytical Chemistrychemistry.chemical_compoundMembraneMicellar liquid chromatographyPhase (matter)Drug DiscoveryMicellar solutionsLipid bilayerMolecular Biologydescription
Solute partitioning into lipid bilayers of biological membranes is the basis for drug and metabolite uptake, passive transport across membranes and bioaccumulation. In order to emulate in vitro the partitioning process in the biomembranes, different approaches have been proposed. The use of micellar solutions as mobile phases in reversed-phase liquid chromatography (micellar liquid chromatography, MLC) has proven to be valid in the prediction of the biological activities of local anesthetics, catecholamines and barbiturates. In this paper we focus our attention on benzodiazepines. The retention of benzodiazepines using different concentrations of Brij35 as micellar mobile phase in modified C18 stationary phase was studied. Quantitative retention–activity relationships (QRAR) in MLC were investigated for these compounds. An adequate correlation between the capacity factors (log k) and the toxicity (log LD50) and anxiolitic activity (log ED50) of benzodiazepines was obtained. Copyright © 1999 John Wiley & Sons, Ltd.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1999-10-01 | Biomedical Chromatography |