Endothelin Receptor Antagonists

The ET receptor antagonist, bosentan (Figure 10) is approved for the treatment of pulmonary hypertension in humans supporting the role of ET in the pathogenesis of this type of hypertension. ETA receptor blockade reduces blood pressure and improves endothelial dysfunction in high-endothelin models of hypertension. For example, ETA receptor blockade attenuated hypertension, oxidative stress, and NADPH oxidase activity during chronic aldosterone-induced hypertension.83 ETA receptor blockade also prolongs survival and reduces proteinuria, but has little effect on the progression of hypertension in salt-loaded stroke-prone spontaneously hypertensive rats.

ET may also have a role in obesity and its associated hypertension. Increased vascular production of ET-1 in hypertensive patients with increased body mass may be a potential mechanism for endothelial dysfunction. ETA receptor-dependent vasoconstrictor tone increased in obese hypertensive patients and blockade of the ETA receptor induced significant vasodilation in overweight and obese humans but not in lean hypertensive subjects. ET receptor antagonism also attenuates elevated blood pressure and reduces renal and cardiac damage in rats fed a high-fructose diet, suggesting that ETreceptor blockers could be a potential approach for treatment of obesity-induced hypertension and renal dysfunction.84

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