On August 15, 2017, Platania, Chiara Bianca Maria; Giurdanella, Giovanni; Di Paola, Luisa; Leggio, Gian Marco; Drago, Filippo; Salomone, Salvatore; Bucolo, Claudio published an article.COA of Formula: C28H32N4O2S The title of the article was P2X7 receptor antagonism: Implications in diabetic retinopathy. And the article contained the following:
Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been demonstrated indicating this receptor as potential pharmacol. target in DR. Here the authors first carried out an in silico mol. modeling study in order to characterize the allosteric pocket in P2X7R, and identify a suitable P2X7R antagonist through mol. docking. JNJ47965567 was identified as the hit compound in docking calculations, as well as for its absorption, distribution, metabolism and excretion (ADME) profile. As an in vitro model of early diabetic retinopathy, human retinal pericytes were exposed to high glucose (25 mM, 48 h) that caused a significant (p < 0.05) release of IL-1β and LDH. The block of P2X7R by JNJ47965567 significantly (p < 0.05) reverted the damage elicited by high glucose, detected as IL-1β and LDH release. Overall, the findings suggest that the P2X7R represents an attractive pharmacol. target to manage the early phase of diabetic retinopathy, and the compound JNJ47965567 is a good template to discover other P2X7R selective antagonists. 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).COA of Formula: C28H32N4O2S
The Article related to p2x7 receptor antagonism diabetic retinopathy, diabetic retinopathy, il-1β, inflammation, molecular modeling, p2x7 receptor, pericytes, Pharmacology: Effects Of Agents For Treating Metabolic and Endocrine Disorders and other aspects.COA of Formula: C28H32N4O2S
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics