Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
Original Article
Quantification of antipsychotic biotransformation in brain microvascular endothelial cells by using untargeted metabolomics
Surachai NgamratanapaiboonPracha Yambangyang
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2021 Volume 15 Issue 6 Pages 317-324


Most studies of antipsychotic-therapies have highlighted the discrepancy between plasma and brain pharmacokinetics of antipsychotics, but how the drug changes through the blood brain barrier (BBB) has not been investigated. Cell-based metabolomics using liquid chromatography-mass spectrometry (LC-MS) combined with multivariate data analysis were applied for screening of antipsychotic metabolites in the BBB. We applied this approach to analyze the antipsychotic biotransformation in brain microvascular endothelia cells (BMVECs), the main component of the BBB. From this study, five, four, three, and one metabolite of chlorpromazine, clozapine, haloperidol and risperidone, respectively, were locally metabolized on the BMVECs. These results confirm that there is a drug biotransformation process within the BBB and show that drug metabolite screening employed cell-based metabolomics using LC-MS, combined with multivariate analysis in the study of BMVECs exposed to antipsychotics can provide a way to screen drug metabolites in the BBB.

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© 2021 International Research and Cooperation Association for Bio & Socio-Sciences Advancement
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