On April 22, 2021, Hopper, Allen T.; Juhl, Martin; Hornberg, Jorrit; Badolo, Lassina; Kilburn, John Paul; Thougaard, Annemette; Smagin, Gennady; Song, Dekun; Calice, Londye; Menon, Veena; Dale, Elena; Zhang, Hong; Cajina, Manuel; Nattini, Megan E.; Gandhi, Adarsh; Grenon, Michel; Jones, Ken; Khayrullina, Tanzilya; Chandrasena, Gamini; Thomsen, Christian; Zorn, Stevin H.; Brodbeck, Robb; Poda, Suresh Babu; Staal, Roland; Moller, Thomas published an article.Related Products of 1428327-31-4 The title of the article was Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. And the article contained the following:
There remains an insufficient number of P2X7 receptor antagonists with adequate rodent potency, CNS permeability, and pharmacokinetic properties from which to evaluate CNS disease hypotheses preclinically. Herein, we describe the mol. pharmacol., safety, pharmacokinetics, and functional CNS target engagement of Lu AF27139, a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. In vivo mouse CNS microdialysis studies of lipopolysaccharide (LPS)-primed and 2′(3′)-O-(benzoylbenzoyl)adenosine-5′-triphosphate (BzATP)-induced IL-1β release demonstrate functional CNS target engagement. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Based on these properties, we believe Lu AF27139 will be a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Related Products of 1428327-31-4
The Article related to orally bioavailable cns penetrant p2x7 receptor antagonist probe, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 1428327-31-4
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