Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2A Inverse Agonists for the Treatment of Insomnia was written by Teegarden, Bradley R.;Li, Hongmei;Jayakumar, Honnappa;Strah-Pleynet, Sonja;Dosa, Peter I.;Selaya, Susan D.;Kato, Naomi;Elwell, Katie H.;Davidson, Jarrod;Cheng, Karen;Saldana, Hazel;Frazer, John M.;Whelan, Kevin;Foster, Jonathan;Espitia, Stephan;Webb, Robert R.;Beeley, Nigel R. A.;Thomsen, William;Morairty, Stephen R.;Kilduff, Thomas S.;Al-Shamma, Hussien A.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 16413-26-6 This article mentions the following:
Insomnia affects a growing portion of the adult population in the U. S. Most current therapeutic approaches to insomnia primarily address sleep onset latency. Through the 5-hydroxytryptamine2A (5-HT2A) receptor, serotonin (5-HT) plays a role in the regulation of sleep architecture, and antagonists/inverse-agonists of 5-HT2A have been shown to enhance slow wave sleep (SWS). We describe here a series of 5-HT2A inverse-agonists that when dosed in rats, both consolidate the stages of NREM sleep, resulting in fewer awakenings, and increase a physiol. measure of sleep intensity. These studies resulted in the discovery of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin)(I), a potent inverse-agonist of 5-HT2A that was advanced into clin. trials for the treatment of insomnia. In the experiment, the researchers used many compounds, for example, 3-Cyanophenylisocyanate (cas: 16413-26-6Recommanded Product: 16413-26-6).
3-Cyanophenylisocyanate (cas: 16413-26-6) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Recommanded Product: 16413-26-6
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