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Urotensin-II GPCR Assays

Background of Urotensin-II Receptors

The urotensin-2 receptor, also known as GPR14, is a class A rhodopsin family G protein-coupled receptor (GPCR) that binds to the neuropeptide urotensin II. The activation of the urotensin-2 receptor would induce the potent vasoconstriction effect and is associated with cardiovascular effects, stress, and REM sleep. The urotensin-II receptor has served as a notable target against various cardiovascular diseases, including heart failure, pulmonary hypertension, and atherosclerosis.

Activation protein kinase C via urotensin-II receptor. Fig.1. Activation protein kinase C via urotensin-II receptor.

Distributions and Functions of Urotensin-II Receptors

Urotensin-II receptors are widely distributed throughout the entire brain. In addition, high-level expression of urotensin-II receptors is also found in the peripheral vasculature, heart, and kidney. The urotensin-II (UT) receptor can mediate complex hemodynamic effects and influence neuromuscular physiology.

Mechanisms of Urotensin-II Receptors

Receptor Gene Mechanism Agonists Antagonists
Urotensin-II receptor UTS2R
  • Urotensin-II receptor activating Protein Kinase C (PKC) via the interaction with Gq/11.
  • The activation of the urotensin-II receptor can promote beta-arrestin translocation.
  • Urotensin-II
  • Urotensin-II related peptide
  • KR-36676
  • KR-36996

Assay List of Urotensin Receptor

Creative Biolabs can provide a range of assays of urotensin receptor. You can choose the assay in the list or contact us for more information:

UTS2R
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX201 Magic™ Human UTS2R In Vitro Calcium Assay, HEK293-Ga15 HEK293-Ga15 Calcium Flux Assay
S01YF-1122-KX982 Magic™ Rat UTS2R In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
IP1 Assay
S01YF-1122-KX980 Magic™ Human UTS2R In Vitro IP1 Assay CHO-K1 IP1 Assay

Published Data

Paper Title Conserved role of the urotensin II receptor 4 signaling pathway to control body straightness in a tetrapod
Journal Open Biology
Published 2021
Abstract Found in teleosts, Urp1 and Urp2 are two neuropeptides of the urotensin II family expressed primarily in neurons exposed to cerebrospinal fluid (CSF). Urp1 and Urp2 are essential for proper shaft formation and maintenance. They are also thought to be mediated by the receptor Uts2r3. It has been shown that loss of uts2r3 causes severe scoliosis in adult zebrafish. In this paper, we report that toad cells containing urp2 mRNA are CSF-contacting neurons. Furthermore, we identified utr4, the X. laevis counterpart of zebrafish uts2r3. Ultimately, we conclude that the role of the Utr4 signaling pathway in the control of body straightness is an ancestral trait of bony vertebrates.
Result Here, we study the urp2 gene in quadrupeds for the first time and find that toad urp2 is predominantly expressed in CSF-contacting neurons of the spinal cord and hindbrain. Through experiments, we also confirmed that utr4 knockout can cause severe axial bending in tadpoles. Ultimately we conclude that the Utr4 signaling pathway plays a role in the control of body straightness not only in ray-finned fishes but also in bony vertebrates. In future studies, we need to further identify new pathogenic mechanisms of IS.

Localization of urotensin II receptor mRNAs in X. laevis embryo revealed by in situ hybridization. Fig.2. Localization of urotensin II receptor (utr) mRNAs in X. laevis embryo revealed by in situ hybridization. (Alejevski, et al., 2021)

Reference

  1. Alejevski, F.; et al. Conserved role of the urotensin II receptor 4 signaling pathway to control body straightness in a tetrapod. Open Biology. 2021, 11(8): 210065.
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