Effect of GSK1016790A, a potent TRPV4 agonist, on lung endothelial permeability
نویسندگان
چکیده
منابع مشابه
Determinants of TRPV4 Activity following Selective Activation by Small Molecule Agonist GSK1016790A
TRPV4 (Transient Receptor Potential Vanilloid 4) channels are activated by a wide range of stimuli, including hypotonic stress, non-noxious heat and mechanical stress and some small molecule agonists (e.g. phorbol ester 4α-PDD). GSK1016790A (GSK101) is a recently discovered specific small molecule agonist of TRPV4. Its effects on physical determinants of TRPV4 activity were evaluated in HeLa ce...
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Transient receptor potential vanilloid receptor 4 (TRPV4) is a calcium-permeable non-selective cation channel implicated in numerous physiological and pathological functions. This study aimed to investigate the effect of TRPV4 activation on respiration and to explore the potential involvement of bronchopulmonary sensory neurons. Potent TRPV4 agonist GSK1016790A was injected into right atrium in...
متن کاملProperties of the Trpv4 Activator Gsk1016790a and the Trpv4 Antagonist Gsk2193874
TO THE EDITOR: We write in response to the recent article by White, Cibelli, Urban, Nilius, McGeown, and Nagy (4). We commend the authors for compiling such a wide literary review on this interesting ion channel, TRPV4. However, we have read with concern the description of the properties of the agonist GSK1016790A and antagonist GSK2193874, and would like to bring the following specific items t...
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The transient receptor potential (TRP) vanilloid subtype 4 (V4) is a nonselective cation channel that exhibits polymodal activation and is expressed in the endothelium, where it contributes to intracellular Ca2+ homeostasis and regulation of cell volume. The purpose of the present study was to evaluate the systemic cardiovascular effects of GSK1016790A, a novel TRPV4 activator, and to examine i...
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TRPV4 ion channel mediates vascular mechanosensitivity and vasodilation. Here, we sought to explore whether non-mechanical activation of TRPV4 could limit vascular inflammation and atherosclerosis. We found that GSK1016790A, a potent and specific small-molecule agonist of TRPV4, induces the phosphorylation and activation of eNOS partially through the AMPK pathway. Moreover, GSK1016790A inhibite...
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ژورنال
عنوان ژورنال: The FASEB Journal
سال: 2010
ISSN: 0892-6638,1530-6860
DOI: 10.1096/fasebj.24.1_supplement.797.5