Cell-Based Radiotracer Binding and Uptake Inhibition Assays: A Comparison of
HEK 293
monoamine
radiotracer
stimulant
synaptosomes
transporter
Journal
Frontiers in pharmacology
ISSN: 1663-9812
Titre abrégé: Front Pharmacol
Pays: Switzerland
ID NLM: 101548923
Informations de publication
Date de publication:
2020
2020
Historique:
received:
18
03
2020
accepted:
24
04
2020
entrez:
9
6
2020
pubmed:
9
6
2020
medline:
9
6
2020
Statut:
epublish
Résumé
High-affinity monoamine transporters are targets for prescribed medications and stimulant drugs of abuse. Therefore, assessing monoamine transporter activity for candidate medications and newly-emerging drugs of abuse provides essential information for industry, academia, and public health. Radiotracer binding and uptake inhibition are the gold standard assays for determining drug-transporter interaction profiles. The combined results from such assays yield a unique biochemical fingerprint for each compound. Over time, different assay methods have been developed to assess transporter activity, and the comparability of data across various assay platforms remains largely unclear. Here, we compare the effects of six well-established stimulants in two different cell-based uptake inhibition assays, one method using adherent cells and the other using suspended cells. Furthermore, we compare the data from transfected cell lines derived from different laboratories and data reported from rat synaptosomes. For transporter inhibitors, IC
Identifiants
pubmed: 32508638
doi: 10.3389/fphar.2020.00673
pmc: PMC7248194
doi:
Types de publication
Journal Article
Langues
eng
Pagination
673Commentaires et corrections
Type : ErratumIn
Informations de copyright
Copyright © 2020 Ilic, Holy, Jaentsch, Liechti, Lubec, Baumann, Sitte and Luethi.
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