6533b7d3fe1ef96bd12614c5
RESEARCH PRODUCT
Efficiency of antidepressant drugs as monoamine reuptake inhibitors: analysis of the hydrophobicity influence using biopartitioning micellar chromatographic data.
M.j. Medina-hernándezC. Quiñones‐torreloSalvador SagradoRosa María Villanueva-camañassubject
Clinical BiochemistryPharmacologyBiochemistrySensitivity and SpecificityAnalytical ChemistryReuptakeStructure-Activity RelationshipDrug DiscoveryBiogenic MonoaminesNeurotransmitter Uptake InhibitorsMolecular BiologyMicellesPharmacologyMolecular interactionsChromatographyChemistryGeneral MedicineAntidepressive AgentsMonoamine neurotransmitterDrug activityAntidepressantSpectrophotometry UltravioletMonoamine reuptake inhibitorPharmacophoreReuptake inhibitorChromatography Liquiddescription
The reuptake blockade of biogenic amines by antidepressants is related not only to their therapeutics effects, but also to their side effects and potential drug-drug interactions. As an alternative to classical quantitative structure-activity relationships studies, in this work we propose different quantitative retention-activity relationships (QRAR) models that are able to describe the monoamine reuptake inhibition by antidepressants. The retention of compounds is measured using a biopartitioning micellar chromatography (BMC) system that can simulate the same hydrophobic, electronic and steric molecular interactions as those that condition drug activity. Since all the compounds considered in this work are structurally related because all of them share the same molecular features as the corresponding basic pharmacophore, the results obtained show that there is a retention range in which antidepressants present the highest monoamine reuptake inhibitor potency.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2004-09-02 | Biomedical chromatography : BMC |