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Improved accuracy of delayed cerebral ischemia diagnosis with plasma nitric oxide synthase 3, nicotinamide adenine dinucleotide phosphate, and 8-iso-prostaglandin F2α.
J Neurosurg
January 2025
4Department of Neurosurgery, Royal Melbourne Hospital, Melbourne, Victoria, Australia.
Objective: The pathophysiology of delayed cerebral ischemia (DCI) is not fully elucidated. The lack of accurate diagnostic tools increases the probability of delayed diagnosis and timely treatment. The authors assessed the relationship of 8-iso-prostaglandin F2α (F2-IsoP) and oxidative stress biomarkers, nitric oxide synthase 3 (NOS3) and nicotinamide adenine dinucleotide phosphate (NADPH), with DCI after aneurysmal subarachnoid hemorrhage (aSAH).
View Article and Find Full Text PDFPhase 1 Mass Balance Study of Pizuglanstat: An Investigational Hematopoietic Prostaglandin D Synthase Inhibitor.
Clin Pharmacol Drug Dev
January 2025
Taiho Pharmaceutical Co., Ltd., Tokyo, Japan.
Pizuglanstat is a novel hematopoietic prostaglandin D synthase inhibitor and investigational treatment for Duchenne muscular dystrophy. This Phase 1 mass balance study aimed to characterize the absorption, metabolism, and excretion of carbon-14 (C)-labeled pizuglanstat in healthy adults (ClinicalTrials.gov, NCT04825431).
View Article and Find Full Text PDFCp40-mediated complement C3 inhibition dampens inflammasome activation and inflammatory mediators storm induced by Bitis arietans venom.
Int Immunopharmacol
January 2025
Immunochemistry Laboratory, Butantan Institute, São Paulo, SP, Brazil; Center of Toxins, Cell Signaling and Immune Response (CeTICS), CEPID, FAPESP, Brazil. Electronic address:
The complement system plays a crucial role in various pathophysiological conditions, including snake envenomation. In this study, we investigated the effects of Bitis arietans venom on the complement system using an ex vivo human whole blood model. Our findings demonstrate that B.
View Article and Find Full Text PDFDevelopment of novel GI-centric prostaglandin E receptor type 4 (EP4) agonist prodrugs as treatment for ulcerative colitis and other intestinal inflammatory diseases.
Bioorg Med Chem Lett
January 2025
Department of Chemistry, Simon Fraser University Burnaby British Columbia Canada. Electronic address:
Prostaglandin E receptor type 4 (EP4) agonists have been shown to be effective in treating experimental ulcerative colitis (UC) in animals and in human clinical trials, but their development has been impeded by unacceptable systemic side effects. In this study, a series of methylene phosphate prodrugs of a highly potent and selective prostaglandin EP4 receptor agonist were designed to target and remain localized in the gastrointestinal (GI) tract after either oral or rectal instillation. The prodrugs were designed to be converted to liberate active EP4 agonist by intestinal alkaline phosphate (IAP), a ubiquitous enzyme found at the luminal of the intestinal wall thus exposing the colon epithelial barrier while reducing systemic exposure to the active agonist.
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