发现N1-(6-氯咪唑并[2,1-b][1,3]噻唑-5-磺酰基)色胺是一种强效、选择性且口服活性的5-羟色胺(6)受体激动剂。
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
作者信息
Cole Derek C, Stock Joseph R, Lennox William J, Bernotas Ronald C, Ellingboe John W, Boikess Steve, Coupet Joseph, Smith Deborah L, Leung Louis, Zhang Guo-Ming, Feng Xidong, Kelly Michael F, Galante Rocco, Huang Pingzhong, Dawson Lee A, Marquis Karen, Rosenzweig-Lipson Sharon, Beyer Chad E, Schechter Lee E
机构信息
Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, New York 10965, USA.
出版信息
J Med Chem. 2007 Nov 15;50(23):5535-8. doi: 10.1021/jm070521y. Epub 2007 Oct 19.
N1-Arylsulfonyltryptamines have been identified as 5-HT6 receptor ligands. In particular, N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine (11q) is a high affinity, potent full agonist (5-HT6 Ki = 2 nM, EC50 = 6.5 nM, Emax = 95.5%). Compound 11q is selective in a panel of over 40 receptors and ion channels, has good pharmacokinetic profile, has been shown to increase GABA levels in the rat frontal cortex, and is active in the schedule-induced polydipsia model for obsessive compulsive disorders.
N1-芳基磺酰基色胺已被鉴定为5-HT6受体配体。特别地，N1-(6-氯咪唑并[2,1-b][1,3]噻唑-5-磺酰基)色胺(11q)是一种高亲和力、强效的完全激动剂(5-HT6 Ki = 2 nM，EC50 = 6.5 nM，Emax = 95.5%)。化合物11q在40多种受体和离子通道中具有选择性，具有良好的药代动力学特征，已被证明可提高大鼠额叶皮质中的GABA水平，并且在强迫症的程序诱导多饮模型中具有活性。
Zotero 插件