Novel benzothiophene H1-antihistamines for the treatment of insomnia was written by Moree, Wilna J.;Jovic, Florence;Coon, Timothy;Yu, Jinghua;Li, Bin-Feng;Tucci, Fabio C.;Marinkovic, Dragan;Gross, Raymond S.;Malany, Siobhan;Bradbury, Margaret J.;Hernandez, Lisa M.;O’Brien, Zhihong;Wen, Jianyun;Wang, Hua;Hoare, Samuel R. J.;Petroski, Robert E.;Sacaan, Aida;Madan, Ajay;Crowe, Paul D.;Beaton, Graham. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 4-Methylpicolinonitrile This article mentions the following:
SAR of lead benzothiophene H1-antihistamine I (R = 2-pyridyl) was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans were identified. Had a suitable human half-life as demonstrated in a human microdose study, but variability in pharmacokinetic profile, attributed to metabolic clearance, prevented further development of this compound I (R = 1-pyrazolyl) demonstrated lower predicted clearance in preclin. studies, and may represent a more suitable backup compound In the experiment, the researchers used many compounds, for example, 4-Methylpicolinonitrile (cas: 1620-76-4Recommanded Product: 4-Methylpicolinonitrile).
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