The differential distribution of ETA and ETB receptors in the human coronary vasculature suggests that ETB receptors in distal regions and microvessels may play a role in coronary syndromes.
May inform selective ETA/ETB antagonist development; leaves open microvascular ETB contributions to coronary syndromes pending human data.
Endothelin (ET)-1 is an endothelium-derived constrictor peptide that is believed to play a pathophysiologic role in coronary artery disease. Receptors for this peptide have been identified on human coronary tissue by in vitro autoradiography. A number of available compounds are selective for ETA or ETB receptors. Here we have used radiolabeled PD 151242 and BQ 3020 to identify ETA and ETB binding sites on sections of human coronary vasculature. ETA receptors are associated with smooth muscle of the coronary artery. Smooth muscle ETB receptor binding is weak at proximal portions of this vessel but increases toward distal regions. ETB receptors are exclusively associated with myocardial capillaries. Our results indicate that, apart from ETA-induced vasoconstriction, stimulation of ETB receptors at distal regions of the coronary vasculature and myocardial microvessels may play an important role in the pathophysiology of coronary syndromes.
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Dashwood et al. (1995) studied this question.
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