January 1, 1996Journal of Cardiovascular Pharmacology
Up-Regulation of Endothelin-B Receptors in Atherosclerotic Human Coronary Arteries
Population
Human coronary arteries from cardiomyopathic hearts, atherosclerotic hearts, one donor heart, and porcine…
Comparison
Competition binding experiments and functional… vs Comparison between atherosclerotic…
Design
Preclinical
Authors
Discussion
Loading...
Member takes
Implication
ETB upregulation may alter coronary vasoreactivity in atherosclerosis; hypothesis-generating for ETB-selective interventions, needs prospective validation.
Key Points
- This research aims to investigate the presence and functional roles of endothelin receptors in human coronary arteries affected by coronary artery disease and cardiomyopathy.
- Competition binding experiments were conducted using [125I]ET-1 with various selective agonists and antagonists.
- Coronary arteries from human cardiomyopathic and atherosclerotic hearts were compared alongside porcine coronary arteries.
- Analysis included receptor density (Bmax), affinity constants (KD), and functional assessments of receptor-mediated responses.
- In human atherosclerotic hearts, ETB receptor levels increased significantly (49% ETB) compared to other groups.
- Total receptor density was highest in porcine arteries (385 fmol/mg), followed by human coronary artery disease (253 fmol/mg) and cardiomyopathy (174 fmol/mg).
- ET-induced constriction in human CMP hearts was mediated solely by ETA receptors, contrasting with porcine arteries.
Structured PICO
P
Population
Human coronary arteries from cardiomyopathic hearts (n=5), atherosclerotic hearts (n=3), one donor heart, and porcine coronary arteries (n=5).
I
Intervention
Competition binding experiments and functional constriction assays using endothelin receptor agonists/antagonists (ET-1, ET-3, Sarafotoxin S6c, BQ-123, bosentan)
C
Comparator
Comparison between atherosclerotic (CAD), cardiomyopathic (CMP), and porcine coronary arteries
O
Outcome
Relative and absolute densities (Bmax) of ETA and ETB receptorssurrogate
ETB receptors are significantly up-regulated in human atherosclerotic coronary arteries compared to cardiomyopathic or healthy tissues, suggesting a potential pathophysiological role in coronary artery disease.
Limitations
- Functional role of ETB receptors in CAD tissue could not be evaluated because of the occurrence of spontaneous phasic contractions.
Cite This Study
Dagassan et al. (1996) studied this question.