Key result
Coexpression of ET(A) and ET(B) receptors in human Girardi heart cells demonstrates intracellular cross-talk, where ET(A) stimulation lowers the affinity of antagonists for ET(B) receptors.
Population
Human Girardi heart cells expressing endothelin ET receptors (GH cells) transfected with human ET cDNA (GH…
Comparison
Endothelin-1 and various antagonists/agonists vs Different combinations of antagonists/agonists…
Design
Preclinical
Authors
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May influence ET antagonist affinity in coexpressing cardiac cells; leaves open in vivo relevance and clinical translation.
The study demonstrates intracellular cross-talk between endothelin ET(A) and ET(B) receptors in human Girardi heart cells, where ET(A) stimulation lowers ET(B) antagonist/agonist affinity.
Ozaki et al. (1997) studied this question. Endothelin receptor antagonists (BQ-123, BQ-3020, BQ-788) was evaluated on Receptor binding affinity, intracellular calcium concentrations, and cAMP accumulation. Coexpression of ET(A) and ET(B) receptors in human Girardi heart cells demonstrates intracellular cross-talk, where ET(A) stimulation lowers the affinity of antagonists for ET(B) receptors.