Abstract
Urotensin-II (U-II) is a "somatostatin-like" cyclic neuropeptide which was originally isolated from goby fish urophysis, and subsequently identified in other species, including man. The interest in human U-II (hU-II) has grown enormously in the last few years, following the identification of a specific human receptor (formerly identified as the GPR14/SENR orphan receptor), now referred to as UT receptor. The U-II/UT system seems to play an important role in cardiovascular functions. hU-II vasoconstrictive potency is reported to be an order of magnitude greater than that of endothelin-1 (ET-1), which would make it the most potent mammalian vasoconstrictor identified to date. hU-II also exerts potent inotropic effects in the human heart in vitro. On the basis of its spectrum of activities, hU-II has been suggested to modulate cardiovascular homeostasis and possibly to be involved in certain cardiovascular pathologies. Central nervous effects of U-II have also been described, in particular, intracerebroventricular administration promotes anxiogenic-like behaviors in rodents. Furthermore, UT receptor overexpression has been observed in some tumor cell lines. Therefore, specific and selective UT receptor antagonists provide useful tools for investigating the (patho)physiological role(s) of the U-II/UT receptor system. In this review we aim to provide an overview of the research in the area of UT receptor antagonists as well as the progress in understanding the role of the UII/ UT system in human (patho)physiology.
Keywords: Urotensin-II, Antagonists, NMR studies, Biological Activity, SAR
Current Medicinal Chemistry
Title: Urotensin-II Receptor Antagonists
Volume: 13 Issue: 3
Author(s): A. Carotenuto, P. Grieco, P. Rovero and E. Novellino
Affiliation:
Keywords: Urotensin-II, Antagonists, NMR studies, Biological Activity, SAR
Abstract: Urotensin-II (U-II) is a "somatostatin-like" cyclic neuropeptide which was originally isolated from goby fish urophysis, and subsequently identified in other species, including man. The interest in human U-II (hU-II) has grown enormously in the last few years, following the identification of a specific human receptor (formerly identified as the GPR14/SENR orphan receptor), now referred to as UT receptor. The U-II/UT system seems to play an important role in cardiovascular functions. hU-II vasoconstrictive potency is reported to be an order of magnitude greater than that of endothelin-1 (ET-1), which would make it the most potent mammalian vasoconstrictor identified to date. hU-II also exerts potent inotropic effects in the human heart in vitro. On the basis of its spectrum of activities, hU-II has been suggested to modulate cardiovascular homeostasis and possibly to be involved in certain cardiovascular pathologies. Central nervous effects of U-II have also been described, in particular, intracerebroventricular administration promotes anxiogenic-like behaviors in rodents. Furthermore, UT receptor overexpression has been observed in some tumor cell lines. Therefore, specific and selective UT receptor antagonists provide useful tools for investigating the (patho)physiological role(s) of the U-II/UT receptor system. In this review we aim to provide an overview of the research in the area of UT receptor antagonists as well as the progress in understanding the role of the UII/ UT system in human (patho)physiology.
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Cite this article as:
Carotenuto A., Grieco P., Rovero P. and Novellino E., Urotensin-II Receptor Antagonists, Current Medicinal Chemistry 2006; 13 (3) . https://dx.doi.org/10.2174/092986706775476061
DOI https://dx.doi.org/10.2174/092986706775476061 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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