Recommanded Product: Ethyl 2-amino-2-thioxoacetateIn 2017 ,《Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists》 was published in Journal of Medicinal Chemistry. The article 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.. The article contains the following contents:
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. The experimental part of the paper was very detailed, including the reaction process of 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. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Recommanded Product: Ethyl 2-amino-2-thioxoacetate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics