Toxicokinetics and analytical toxicology of the abused opioid U-48800 - in vitro metabolism, metabolic stability, isozyme mapping, and plasma protein binding.
Analgesics, Opioid
/ blood
Animals
Blood Proteins
/ metabolism
Cytochrome P-450 CYP2C19
/ metabolism
Cytochrome P-450 CYP3A
/ metabolism
Designer Drugs
/ metabolism
Humans
Isoenzymes
/ metabolism
Male
Microsomes, Liver
/ drug effects
Protein Binding
Rats, Wistar
Substance Abuse Detection
Tandem Mass Spectrometry
Toxicokinetics
LC−HRMS/MS
metabolic stability
new synthetic opioids
pooled human liver S9 fraction
Journal
Drug testing and analysis
ISSN: 1942-7611
Titre abrégé: Drug Test Anal
Pays: England
ID NLM: 101483449
Informations de publication
Date de publication:
Oct 2019
Oct 2019
Historique:
received:
11
06
2019
revised:
02
08
2019
accepted:
14
08
2019
pubmed:
20
8
2019
medline:
27
2
2020
entrez:
20
8
2019
Statut:
ppublish
Résumé
Due to the risk of new synthetic opioids (NSOs) for human health, the knowledge of their toxicokinetic characteristics is important for clinical and forensic toxicology. U-48800 is an NSO structurally non-related to classical opioids such as morphine or fentanyl and offered for abuse. As toxicokinetic data of U-48800 is not currently available, the aims of this study were to identify the in vitro metabolites of U-48800 in pooled human liver S9 fraction (pS9), to map the isozymes involved in the initial metabolic steps, and to determine further toxicokinetic data such as metabolic stability, including the in vitro half-life (t
Substances chimiques
Analgesics, Opioid
0
Blood Proteins
0
Designer Drugs
0
Isoenzymes
0
Cytochrome P-450 CYP2C19
EC 1.14.14.1
Cytochrome P-450 CYP3A
EC 1.14.14.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1572-1580Informations de copyright
© 2019 The Authors. Drug Testing and Analysis published by John Wiley & Sons Ltd.
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