Search Results - "Costell, Melissa H"
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Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress
Published in Frontiers in pharmacology (01-01-2012)“…Soluble guanylate cyclase (sGC), the primary mediator of nitric oxide (NO) bioactivity, exists as reduced (NO-sensitive) and oxidized (NO-insensitive) forms…”
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Evaluation of GSK2789917-induced TRPV4 inhibition in animal models of fluid induced lung injury
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-05-2024)“…Administration of bolus intravenous fluids, common in pre-hospital and hospitalised patients, is associated with increased lung vascular permeability and…”
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Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid‑4 (TRPV4)
Published in Journal of medicinal chemistry (08-11-2018)“…A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported…”
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Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo
Published in The Journal of pharmacology and experimental therapeutics (01-03-2021)“…Transient receptor potential vanilloid 4 (TRPV4) channels expressed on pulmonary endothelial cells are activated by elevated pulmonary vascular pressure,…”
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Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid‑4 (TRPV4)
Published in Journal of medicinal chemistry (24-10-2019)“…GSK3527497, a preclinical candidate for the inhibition of TRPV4, was identified starting from the previously reported pyrrolidine sulfonamide TRPV4 inhibitors…”
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Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid‑4 with in Vivo Activity in a Pulmonary Edema Model
Published in Journal of medicinal chemistry (27-12-2018)“…Pulmonary edema is a common ailment of heart failure patients and has remained an unmet medical need due to dose-limiting side effects associated with current…”
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Chronic Inhibition of 11β-Hydroxysteroid Dehydrogenase Type 1 Activity Decreases Hypertension, Insulin Resistance, and Hypertriglyceridemia in Metabolic Syndrome
Published in BioMed research international (01-01-2013)“…Metabolic syndrome is a constellation of risk factors including hypertension, dyslipidemia, insulin resistance, and obesity that promote the development of…”
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Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase
Published in Bioorganic & medicinal chemistry letters (15-06-2013)“…1-(1,3,5-Triazin-yl)piperidine-4-carboxamide inhibitors of soluble epoxide hydrolase were identified from high through-put screening using encoded library…”
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Modulation of transient receptor potential canonical channel 3 (TRPC3) activity by a novel pharmacological agonist and antagonist in normotensive and hypertensive rats
Published in The FASEB journal (01-04-2012)“…Abstract only Transient receptor potential canonical channel 3 (TRPC3) is a nonselective cation channel that is associated with hypertension. Previous studies…”
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Sodium and water homeostasis is maintained in rats with chronic TRPV4 blockade
Published in The FASEB journal (01-04-2011)“…The transient receptor potential vanilloid 4 (TRPV4) is a non‐selective cation channel that highly expressed in renal tubules. Co‐localization of TRPV4 with…”
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Activation of nitric oxide (NO)‐insensitive soluble guanylate cyclase does not provide greater benefit than NO‐sensitive stimulation in acute and chronic models of cardiovascular disease associated with oxidative stress
Published in The FASEB journal (01-04-2011)“…Soluble guanylate cyclase (sGC), the primary mediator of nitric oxide (NO), exists as reduced (NO‐sensitive) and oxidized (NO‐insensitive) forms. Because…”
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12
Serum and glucocorticoid‐regulated kinase mediates hypertension and end organ damage in DOCA‐salt hypertension
Published in The FASEB journal (01-03-2008)“…Abstract only Serum and glucocorticoid‐regulated kinase 1 (SGK1) plays an important role in mediating mineralocorticoid receptor stimulated sodium…”
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Chronic inhibition of 11beta‐hydroxysteroid dehydrogenase activity reduces cardiovascular comorbidities in corpulent and stroke‐prone SHR
Published in The FASEB journal (01-03-2008)“…Abstract only Changes in the secretion or metabolism of cortisol are associated with human hypertension and metabolic disorders. 11beta‐hydroxysteroid…”
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Compensatory role for Sgk2 mediated sodium reabsorption during salt deprivation in Sgk1 knockout mice
Published in The FASEB journal (01-04-2007)“…The purpose of this study was to investigate the role of Sgk2 in the regulation of salt and water homeostasis. Kidney function and expression of Sgk1, Sgk2,…”
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