Contribution of Monocarboxylate Transporter 6 to the Pharmacokinetics and Pharmacodynamics of Bumetanide in Mice.
Administration, Intravenous
Administration, Oral
Animals
Bumetanide
/ administration & dosage
Diuresis
/ drug effects
Drug Evaluation, Preclinical
Kidney Cortex
/ drug effects
Male
Mice
Mice, Knockout
Monocarboxylic Acid Transporters
/ genetics
Oocytes
Recombinant Proteins
/ genetics
Sodium Potassium Chloride Symporter Inhibitors
/ administration & dosage
Xenopus laevis
Journal
Drug metabolism and disposition: the biological fate of chemicals
ISSN: 1521-009X
Titre abrégé: Drug Metab Dispos
Pays: United States
ID NLM: 9421550
Informations de publication
Date de publication:
09 2020
09 2020
Historique:
received:
07
04
2020
accepted:
08
06
2020
pubmed:
27
6
2020
medline:
14
9
2021
entrez:
27
6
2020
Statut:
ppublish
Résumé
Bumetanide, a sulfamyl loop diuretic, is used for the treatment of edema in association with congestive heart failure. Being a polar, anionic compound at physiologic pH, bumetanide uptake and efflux into different tissues is largely transporter-mediated. Of note, organic anion transporters (SLC22A) have been extensively studied in terms of their importance in transporting bumetanide to its primary site of action in the kidney. The contribution of one of the less-studied bumetanide transporters, monocarboxylate transporter 6 (MCT6; SLC16A5), to bumetanide pharmacokinetics (PK) and pharmacodynamics (PD) has yet to be characterized. The affinity of bumetanide for murine Mct6 was evaluated using Mct6-transfected
Identifiants
pubmed: 32587098
pii: dmd.120.000068
doi: 10.1124/dmd.120.000068
pmc: PMC7469248
doi:
Substances chimiques
Monocarboxylic Acid Transporters
0
Recombinant Proteins
0
Slc16a5 protein, mouse
0
Sodium Potassium Chloride Symporter Inhibitors
0
Bumetanide
0Y2S3XUQ5H
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
788-795Subventions
Organisme : NIDA NIH HHS
ID : R01 DA023223
Pays : United States
Informations de copyright
Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics.
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