Dataset Information
Kinetics of endothelin-1 and effect selective ET<sub>A</sub> antagonism on ET<sub>B</sub> activation: a mathematical modeling analysis.
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ABSTRACT: Introduction
Endothelin-1 (ET-1) regulates renal and vascular function, but the clinical utility of selective ETA receptor antagonists has been limited due to associated fluid retention. The mechanisms underlying fluid retention remain poorly understood but could be a consequence of changes in ET-1 binding to the unantagonized ETB receptor, either through increased ET-1 or non-selective ETB.Methods
A mathematical model of ET-1 kinetics was developed to quantify effects of ETA antagonist exposure and selectivity on concentrations of ET-1 and its complexes with ETA and ETB receptors. The model describes ET-1 production, tissue and plasma distribution, ETA and ETB receptor binding, and rece
SUBMITTER: Hallow KM
PROVIDER: S-EPMC11632605 | biostudies-literature | 2024
REPOSITORIES: biostudies-literature