Urotensin-II and the cardiovascular system--the importance of developing modulators

Urotensin-II (U-II) potently contracts some large isolated blood vessels and cardiac tissue. However, the maximum effects on human blood vessels and heart are relatively small. U-II dilates human resistance arteries. It markedly decreased myocardial function and increased vascular resistance in cynomolgus monkeys, but the major effects of U-II have not been observed in healthy humans. A major role for U-II in human cardiovascular disease has not been clearly established despite studies in patients with coronary artery disease, heart failure, essential hypertension and diabetes. Peptide and non-peptide agonists and antagonists of the U-II receptor are being developed and will be useful in the characterisation of the effects of U-II, and may have some therapeutic potential.