0000000000181433

AUTHOR

Helena Carmo

0000-0002-6650-5285

showing 3 related works from this author

Metabolic pathways of 4-bromo-2,5-dimethoxyphenethylamine (2C-B): analysis of phase I metabolism with hepatocytes of six species including human

2004

Abstract 4-Bromo-2,5-dimethoxyphenethylamine (2C-B) is a psychoactive designer drug of abuse that is sold under the street names “Venus”, “Bromo”, “Erox”, “XTC” or “Nexus”. Concern has been raised because only little is known about its toxicity and metabolism in humans. In the present study we incubated 2C-B with human, monkey, dog, rabbit, rat and mouse hepatocytes to identify the metabolites formed and to determine possible toxic effects as evidenced by an ATP assay. Our data allow construction of the main metabolic pathways of 2C-B. Oxidative deamination results in the 2-(4-bromo-2,5-dimethoxyphenyl)-ethanol (BDMPE) and 4-bromo-2,5-dimethoxyphenylacetic acid (BDMPAA) metabolites. Additio…

MaleMetaboliteDeaminationMice Inbred StrainsBiologyToxicologyGas Chromatography-Mass SpectrometryRats Sprague-DawleyMicechemistry.chemical_compoundAdenosine TriphosphateDogsSpecies SpecificitymedicineAnimalsHumansCells CulturedDemethylationDose-Response Relationship DrugMolecular Structure25-Dimethoxy-4-MethylamphetamineIllicit DrugsOxidative deaminationMetabolismMiddle AgedRatsMacaca fascicularisMetabolic pathwaymedicine.anatomical_structurechemistryBiochemistryDeaminationHepatocyteHepatocytesRabbitsOxidation-ReductionDrug metabolismToxicology
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CYP2D6 increases toxicity of the designer drug 4-methylthioamphetamine (4-MTA)

2006

4-Methylthioamphetamine (4-MTA) belongs to a group of new amphetamine derivatives that is usually sold as "ecstasy" or "flatliners" on the illicit drug market. Large interindividual differences in 4-MTA mediated toxicity have been reported in humans. Therefore, we tested whether CYP2D6 or its variant alleles as well as CYP3A4 influence the susceptibility to 4-MTA. For this purpose, we used the colony formation assay with Chinese hamster lung fibroblast V79 cells expressing human wild-type CYP2D6 (CYP2D6*1), the low activity alleles CYP2D6*2, CYP2D6*9, as well as human CYP3A4. The obtained results showed that the expression of wild type CYP2D6*1 clearly enhanced the susceptibility to the cyt…

GenotypeCYP3A4Cell SurvivalAmphetaminesWild typePharmacologyBiologyToxicologybiology.organism_classificationIsozymedigestive systemChinese hamsterCell LineDesigner DrugsCricetulusCytochrome P-450 CYP2D6Cell cultureCricetinaeToxicityGenotypeAnimalsCytochrome P-450 CYP3ACytotoxic T cellskin and connective tissue diseasesToxicology
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Influence of CYP2D6 polymorphism on the cytotoxicity of the designer drug 4-methylthioamphetamine (4-MTA)

2007

Designer drugCyp2d6 polymorphism4-MethylthioamphetamineChemistrymedicine.drug_classmedicineGeneral MedicinePharmacologyToxicologyCytotoxicitymedicine.drugToxicology Letters
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