Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists was written by Carpenter, Joseph;Wang, Ying;Wu, Gang;Feng, Jianxin;Ye, Xiang-Yang;Morales, Christian L.;Broekema, Matthias;Rossi, Karen A.;Miller, Keith J.;Murphy, Brian J.;Wu, Ginger;Malmstrom, Sarah E.;Azzara, Anthony V.;Sher, Philip M.;Fevig, John M.;Alt, Andrew;Bertekap, Robert L.;Cullen, Mary Jane;Harper, Timothy M.;Foster, Kimberly;Luk, Emily;Xiang, Qian;Grubb, Mary F.;Robl, Jeffrey A.;Wacker, Dean A.. And the article was included in Journal of Medicinal Chemistry in 2017.Synthetic Route of C8H11NO2 This article mentions the following:
Agonism of the 5-HT2C receptor represents one of the most well-studied and clin. proven mechanisms for pharmacol. weight reduction Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been shown to lead to undesirable side effects and major safety concerns. In this communication, we report the development of a new screening paradigm that utilizes an active site mutant D134A (D3.32) 5-HT2C receptor to identify atypical agonist structures. We addnl. report the discovery and optimization of a novel class of nonbasic heterocyclic amide agonists of 5-HT2C. SAR investigations around the screening hits provided a diverse set of potent agonists at 5-HT2C with high selectivity over the related 5-HT2A and 5-HT2B receptor subtypes. Further optimization through replacement of the amide with a variety of five- and six-membered heterocycles led to the identification of 6-(1-ethyl-3-(quinolin-8-yl)-1H-pyrazol-5-yl)pyridazin-3-amine (69). Oral administration of 69 to rats reduced food intake in an ad libitum feeding model, which could be completely reversed by a selective 5-HT2C antagonist. In the experiment, the researchers used many compounds, for example, Ethyl 4-methyl-1H-pyrrole-3-carboxylate (cas: 2199-49-7Synthetic Route of C8H11NO2).
Ethyl 4-methyl-1H-pyrrole-3-carboxylate (cas: 2199-49-7) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 绾?valerolactone.Synthetic Route of C8H11NO2
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics