A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.
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http://dx.doi.org/10.1021/jm700949w | DOI Listing |
Sci Rep
January 2025
Department of Neurosurgery and Brain Research Institute, Yonsei University College of Medicine, Seoul, Republic of Korea.
Although low-intensity focused ultrasound (LiFUS) with microbubbles is used to temporally open the blood-brain barrier (BBB), the underlying mechanism is not fully understood. This study aimed to analyze BBB-related alterations in the brain microenvironment after LiFUS, with a focus on the involvement of the purinergic P × receptor. Sprague-Dawley rats were sonicated with LiFUS at 0.
View Article and Find Full Text PDFNeuropharmacology
January 2025
Dept. of Biomedical and Biotechnological Sciences, Section of Pharmacology, University of Catania, Catania, Italy. Electronic address:
The central nervous system is a well-known steroidogenic tissue producing, among others, cholesterol metabolites such as neuroactive steroids, oxysterols and steroid hormones. It is well known that these endogenous molecules affect several receptor classes, including ionotropic GABAergic and NMDA glutamatergic receptors in neurons. It has been shown that also ionotropic purinergic (P2X) receptors are cholesterol metabolites' targets.
View Article and Find Full Text PDFBioorg Med Chem
December 2024
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, United States. Electronic address:
The purinergic P2X ligand-gated ion channel 7 receptor (P2X7R) plays a critical role in various inflammatory processes and other diseases. Fast determination of compounds P2X7R binding potency and discovery of a promise PET radiotracer for imaging P2X7R require a P2X7R suitable radioligand for radioactive competitive binding assay. Herein, we designed and synthesized thirteen new P2X7R ligands and determined the in vitro binding potency.
View Article and Find Full Text PDFSci Rep
December 2024
Department of Gastroenterology, The Second Affiliated Hospital, Jiangxi Medical College, Nanchang University, Nanchang city, Jiangxi province, China.
Mol Genet Genomics
December 2024
Department of Cardiovascular Medicne, The Second Affiliated Hospital of Nanchang University, No.1 Minde Road, Nanchang, 330006, P.R. China.
Our study examined the relationships and interactions among 30 genes related to the NOD-like receptor protein 3 (NLRP3) inflammasome. We identified 368 interconnections between these 30 genes, with NLRP3 participating in 38 interactions. The potential roles of these genes in atherosclerosis were evaluated based on protein-protein interaction networks and coexpression analysis.
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