Reference of 5117-12-4, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 5117-12-4, Name is 4-Acryloylmorpholine, SMILES is C=CC(=O)N1CCOCC1, belongs to Triazoles compound. In a article, author is Peng, Youyi, introduce new discover of the category.
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management
The sigma 1 receptor (S1R) is a molecular chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathological disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design strategies, we rationally designed, synthesized, and biologically evaluated a series of novel triazole-based SIR antagonists. Compound 10 exhibited potent binding affinity for S1R, high selectivity over S2R and 87 other human targets, acceptable in vitro metabolic stability, slow clearance in liver microsomes, and excellent blood-brain barrier permeability in rats. Further in vivo studies in rats showed that 10 exhibited negligible acute toxicity in the rotarod test and statistically significant analgesic effects in the formalin test for acute inflammatory pain and paclitaxel-induced neuropathic pain models during cancer chemotherapy. These encouraging results promote further development of our triazole-based S1R antagonists as novel treatments for pain of different etiologies.
Reference of 5117-12-4, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 5117-12-4.