Detailed Explanation
Cyclic peptide (11 amino acids in humans, with a disulfide bridge) identified as the most potent vasoconstrictor known — approximately 10× more potent than endothelin-1. Originally discovered in fish urophysis (caudal neurosecretory system), the human form was identified in 1999. Urotensin II acts through the UT receptor (GPR14) expressed in cardiovascular tissue, kidney, and brain.
It is implicated in heart failure, pulmonary hypertension, atherosclerosis, diabetes, and kidney disease, where its levels are elevated. UT receptor antagonists (palosuran) have been investigated for diabetic nephropathy but clinical results have been mixed. Urotensin II also has mitogenic effects, promoting smooth muscle cell proliferation.
Key Facts
- Cyclic peptide (11 amino acids in humans, with a disulfide bridge) identified as the most potent vasoconstrictor known — approximately 10× more potent than endothelin-1.
- Originally discovered in fish urophysis (caudal neurosecretory system), the human form was identified in 1999.
- Urotensin II acts through the UT receptor (GPR14) expressed in cardiovascular tissue, kidney, and brain.
- It is implicated in heart failure, pulmonary hypertension, atherosclerosis, diabetes, and kidney disease, where its levels are elevated.
- UT receptor antagonists (palosuran) have been investigated for diabetic nephropathy but clinical results have been mixed.
- Urotensin II also has mitogenic effects, promoting smooth muscle cell proliferation.
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