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Randomized trial to assess worsening renal function by adding dapagliflozin for acute decompensated heart failure.
ESC Heart Fail
January 2025
Division of Cardiology, Osaka Rosai Hospital, Osaka, Japan.
Aims: Dapagliflozin (DAPA), a sodium-glucose co-transporter 2 inhibitor, has been shown to reduce cardiovascular mortality among patients with chronic heart failure. We aimed to evaluate the impact on a worsening renal function (WRF) by adding DAPA as compared to standard decongestive therapy with loop diuretics alone.
Methods And Results: We enrolled 114 consecutive acute decompensated heart failure (ADHF) patients with a left ventricular ejection fraction (LVEF) of less than 50%.
Single- and multiple-dose pharmacokinetics and safety of the SARS-CoV-2 3CL protease inhibitor RAY1216: a phase 1 study in healthy participants.
Antimicrob Agents Chemother
January 2025
Department of Pediatrics, First Hospital of Jilin University, Changchun, China.
Coronavirus disease 2019, which leads to pneumonia, is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). RAY1216 is a 3C-like protease inhibitor that targets SARS-CoV-2. The aim of our study was to assess the pharmacokinetics (PK) and safety of RAY1216 in healthy volunteers.
View Article and Find Full Text PDFForsythiaside A Ameliorates Inflammation by Regulating the Autophagy in Methotrexate-induced Intestinal Mucositis.
Comb Chem High Throughput Screen
January 2025
Hebei Key Laboratory of Specialty Animal Germplasm Resources Exploration and Innovation, College of Animal Science and Technology, Hebei Normal University of Science and Technology, Qinhuangdao, China.
Background: Methotrexate (MTX) effectively eliminates cancerous cells but can also cause inflammation intestinal, known as mucositis. Forsythiaside A (FTA) from Forsythia suspensa has shown promise in relieving mucositis by targeting the NLRP3 pathways. Since NLRP3 inflammasome activation is negatively regulated by autophagy, this study explores how FTAmediated autophagy affects NLRP3 inflammasome in treating MTX-induced intestinal inflammation.
View Article and Find Full Text PDFDiscovery of Pyrrolopyrazine Carboxamide Derivatives as Potent and Selective FGFR2/3 Inhibitors that Overcome Mutant Resistance.
J Med Chem
January 2025
Insilico Medicine Shanghai Ltd, Suite 901, Tower C, Changtai Plaza, 2889 Jinke Road, Pudong New District, Shanghai 201203, China.
Fibroblast growth factor receptors (FGFRs) are established oncogenic drivers in various solid tumors. However, the approved FGFR inhibitors face challenges with acquired resistance and dose-limiting adverse effects associated with FGFR1/4 inhibition, limiting therapeutic efficacy. Herein, we systematically explored linker and electrophile moieties based on the pyrrolopyrazine carboxamide core and identified aniline α-fluoroacrylamide as an effective covalent warhead.
View Article and Find Full Text PDFUrsodeoxycholic acid protects against sepsis-induced acute kidney injury by activating Nrf2/HO-1 and inhibiting NF-κB pathway.
BMC Nephrol
January 2025
Department of Intensive Care Medicine, No. 971st Hospital of the People's Liberation Army Navy, Qingdao, Shandong Province, PR China.
Background: Ursodeoxycholic acid (UDCA), traditionally recognized for its hepatoprotective effects, has also shown potential in protecting kidney injury. This study aimed to evaluate the protective effects of UDCA against sepsis-induced acute kidney injury (AKI) and to elucidate the underlying mechanisms.
Methods: Sixty male C57BL/6 N mice were utilized to establish a sepsis-induced AKI model through intravenous injection of lipopolysaccharides (LPS, 10 mg/kg).
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