Peng, Youyi; Zhang, Qiang; Welsh, William J. published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management》.Recommanded Product: Ethyl 2-amino-2-thioxoacetate The article contains the following contents:
The sigma 1 receptor (S1R) is a mol. chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathol. disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design strategies, we rationally designed, synthesized, and biol. evaluated a series of novel triazole-based S1R antagonists. In particular, aryl(pyrrolidinylmethyl)triazole I 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 I 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. In the experiment, the researchers used many compounds, for example, Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Recommanded Product: Ethyl 2-amino-2-thioxoacetate)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Recommanded Product: Ethyl 2-amino-2-thioxoacetate
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