Potential Clinical Implications of the Urotensin II Receptor Antagonists
Urotensin-II (UII), which binds to its receptor UT, plays an important role in the heart, kidneys, pancreas, adrenal gland and CNS. In the vasculature, it acts as a potent endothelium-independent vasoconstrictor and endothelium-dependent vasodilator. In disease states, this constriction-dilation equ...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2011-07-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fphar.2011.00038/full |
| _version_ | 1831522921426714624 |
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| author | Emilie Kane Adel Giaid |
| author_facet | Emilie Kane Adel Giaid |
| author_sort | Emilie Kane |
| collection | DOAJ |
| description | Urotensin-II (UII), which binds to its receptor UT, plays an important role in the heart, kidneys, pancreas, adrenal gland and CNS. In the vasculature, it acts as a potent endothelium-independent vasoconstrictor and endothelium-dependent vasodilator. In disease states, this constriction-dilation equilibrium is disrupted. There is an upregulation of the UII system in heart disease, metabolic syndrome and kidney failure. The increase in UII release and UT expression suggest that UII system may be implicated in the pathology and pathogenesis of these diseases by causing an increase in ACAT-1 activity leading to SMC proliferation and foam cell infiltration, insulin resistance (DMII), as well as inflammation, high blood pressure and plaque formation. Recently, UT antagonists such as SB-611812, palosuran, and most recently a piperazino-isoindolinone based antagonist have been developed in the hope of better understanding the UII system and treating its associated diseases. |
| first_indexed | 2024-12-14T04:45:46Z |
| format | Article |
| id | doaj.art-00d0617748ba430392baf95d74adaf64 |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-12-14T04:45:46Z |
| publishDate | 2011-07-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-00d0617748ba430392baf95d74adaf642022-12-21T23:16:41ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122011-07-01210.3389/fphar.2011.000382162Potential Clinical Implications of the Urotensin II Receptor AntagonistsEmilie Kane0Adel Giaid1McGill UniversityMcGill UniversityUrotensin-II (UII), which binds to its receptor UT, plays an important role in the heart, kidneys, pancreas, adrenal gland and CNS. In the vasculature, it acts as a potent endothelium-independent vasoconstrictor and endothelium-dependent vasodilator. In disease states, this constriction-dilation equilibrium is disrupted. There is an upregulation of the UII system in heart disease, metabolic syndrome and kidney failure. The increase in UII release and UT expression suggest that UII system may be implicated in the pathology and pathogenesis of these diseases by causing an increase in ACAT-1 activity leading to SMC proliferation and foam cell infiltration, insulin resistance (DMII), as well as inflammation, high blood pressure and plaque formation. Recently, UT antagonists such as SB-611812, palosuran, and most recently a piperazino-isoindolinone based antagonist have been developed in the hope of better understanding the UII system and treating its associated diseases.http://journal.frontiersin.org/Journal/10.3389/fphar.2011.00038/fullHeartmetabolic syndromekidenysUT |
| spellingShingle | Emilie Kane Adel Giaid Potential Clinical Implications of the Urotensin II Receptor Antagonists Frontiers in Pharmacology Heart metabolic syndrome kidenys UT |
| title | Potential Clinical Implications of the Urotensin II Receptor Antagonists |
| title_full | Potential Clinical Implications of the Urotensin II Receptor Antagonists |
| title_fullStr | Potential Clinical Implications of the Urotensin II Receptor Antagonists |
| title_full_unstemmed | Potential Clinical Implications of the Urotensin II Receptor Antagonists |
| title_short | Potential Clinical Implications of the Urotensin II Receptor Antagonists |
| title_sort | potential clinical implications of the urotensin ii receptor antagonists |
| topic | Heart metabolic syndrome kidenys UT |
| url | http://journal.frontiersin.org/Journal/10.3389/fphar.2011.00038/full |
| work_keys_str_mv | AT emiliekane potentialclinicalimplicationsoftheurotensiniireceptorantagonists AT adelgiaid potentialclinicalimplicationsoftheurotensiniireceptorantagonists |