Microsome Mediated in Vitro Metabolism: A Convenient Method for the Preparation of the PET Radioligand Metabolite [
Fe-PE2I
PET
biotransformation
dopamine transporter
metabolism
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
18 10 2023
18 10 2023
Historique:
medline:
23
10
2023
pubmed:
27
9
2023
entrez:
27
9
2023
Statut:
ppublish
Résumé
Undesired radiometabolites can be detrimental to the development of positron emission tomography (PET) radioligands. Methods for quantifying radioligand metabolites in brain tissue include ex vivo studies in small animals or labeling and imaging of the radiometabolite(s) of interest. The latter is a time- and resource-demanding process, which often includes multistep organic synthesis. We hypothesized that this process could be replaced by making use of liver microsomes, an in vitro system that mimics metabolism. In this study, rat liver microsomes were used to prepare radiometabolites of the dopamine transporter radioligand [
Identifiants
pubmed: 37753876
doi: 10.1021/acschemneuro.3c00458
pmc: PMC10587862
doi:
Substances chimiques
Dopamine Plasma Membrane Transport Proteins
0
Radiopharmaceuticals
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
3732-3736Références
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