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6-Furopyridine Hexamethylene Amiloride Is a Non-Selective P2X7 Recepto by Peter Cuthbertson, Amal Elhage et al

P2X7 is an extracellular adenosine 5′-triphopshate (ATP)-gated cation channel present on leukocytes, where its activation induces pro-inflammatory cytokine release and ectodomain shedding of cell surface molecules. Human P2X7 can be partially inhibited by amiloride and its derivatives at micromolar concentrations. This study aimed to screen a library of compounds derived from amiloride or its derivative 5-(N,N-hexamethylene) amiloride (HMA) to identify a potential P2X7 antagonist. 6-Furopyridine HMA (6-FPHMA) was identified as a novel P2X7 antagonist and was characterized further. 6-FPHMA impaired ATP-induced dye uptake into human RPMI8226 multiple myeloma cells and human P2X7-HEK293 cells, in a concentration-dependent, non-competitive manner. Likewise, 6-FPHMA blocked ATP-induced Ca2+ fluxes in human P2X7-HEK293 cells in a concentration-dependent, non-competitive manner. 6-FPHMA inhibited ATP-induced dye uptake into human T cells, and interleukin-1β release within human blood and C

Immune cell defect tied to the risk of developing rare bacterial infection

Multiomic comparison shows a reduction in circulating monocytes correlated with persistent post-COVID-19 pulmonary fibrosis

In a new study, researchers identified distinguishing immune features of coronavirus disease 2019 (COVID-19) in patients with late-resolving pulmonary fibrosis (LR COVID-PF) and early-resolving (ER COVID-PF).

The impact of sleep fragmentation on the clonal diversity of immune cells and the genetic aging of the hematopoietic system

A new study shows that sleep does much more, regulating the normal production of blood cells. This finding underlines how essential a healthy sleep routine is for a normal life.

A good night s sleep promotes immunity

In a recent study published in the Journal of Experimental Medicine, researchers in the United States used mice models to understand how sleep fragmentation affects immunological responses and the epigenetic modifications of hematopoietic stem and progenitor cells (HSPCs). They also conducted a sleep restriction trial in humans to determine HPSC programming and hematopoiesis.

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