Title
In vitro Phase I and Phase II metabolism of alpha-pyrrolidinovalerophenone (alpha-PVP), methylenedioxypyrovalerone (MDPV) and methedrone by human liver microsomes and human liver cytosol In vitro Phase I and Phase II metabolism of alpha-pyrrolidinovalerophenone (alpha-PVP), methylenedioxypyrovalerone (MDPV) and methedrone by human liver microsomes and human liver cytosol
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Berlin ,
Subject
Chemistry
Biology
Source (journal)
Analytical and bioanalytical chemistry. - Berlin, 2002, currens
Volume/pages
407(2015) :19 , p. 5803-5816
ISSN
1618-2642
ISI
000358136900024
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
The aim of the present study was to identify the in vitro Phase I and Phase II metabolites of three new psychoactive substances: alpha-pyrrolidinovalerophenone (alpha-PVP), methylenedioxypyrovalerone (MDPV), and methedrone, using human liver microsomes and human liver cytosol. Accurate-mass spectra of metabolites were obtained using liquid chromatography-quadrupole time-of-flight mass spectrometry. Six Phase I metabolites of alpha-PVP were identified, which were formed involving reduction, hydroxylation, and pyrrolidine ring opening reactions. The lactam compound was the major metabolite observed for alpha-PVP. Two glucuronidated metabolites of alpha-PVP, not reported in previous in vitro studies, were further identified. MDPV was transformed into 10 Phase I metabolites involving reduction, hydroxylation, and loss of the pyrrolidine ring. Also, six glucuronidated and two sulphated metabolites were detected. The major metabolite of MDPV was the catechol metabolite. Methedrone was transformed into five Phase I metabolites, involving N- and O-demethylation, hydroxylation, and reduction of the ketone group. Three metabolites of methedrone are reported for the first time. In addition, the contribution of individual human CYP enzymes in the formation of the detected metabolites was investigated.
E-info
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https://repository.uantwerpen.be/docman/iruaauth/6a358a/a18127156.pdf
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Full text (open access)
https://repository.uantwerpen.be/docman/irua/e3e99d/127156_2016_07_01.pdf
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