含有哌嗪核心与取代芳基磺酰胺的促黑素皮质素4型受体激动剂。
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
作者信息
Fotsch Christopher, Han Nianhe, Arasasingham Premilla, Bo Yunxin, Carmouche Michelle, Chen Ning, Davis James, Goldberg Martin H, Hale Clarence, Hsieh Feng-Yin, Kelly Michael G, Liu Qingyian, Norman Mark H, Smith Duncan M, Stec Markian, Tamayo Nuria, Xi Ning, Xu Shimin, Bannon Anthony W, Baumgartner James W
机构信息
Department of Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Mailstop 29-1-B, Thousand Oaks, CA 91320, USA.
出版信息
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060.
The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM. The most selective compound in this series was >25,000-fold more potent at MC4R than MC3R, and 490-fold more potent at MC4R than MC5R. This compound also reduced food intake after oral dosing at 25, 50, and 100 mg kg(-1) in fasted mice.
描述了一组含有哌嗪核心并带有邻位取代芳基磺酰胺的促黑素皮质素-4受体（MC4R）激动剂的生物活性。该组化合物在MC4R上的结合和功能活性小于30 nM。该系列中最具选择性的化合物对MC4R的效力比对MC3R高>25,000倍，对MC4R的效力比对MC5R高490倍。该化合物在禁食小鼠中口服给药25、50和100 mg kg(-1)后也能减少食物摄入量。
Zotero 插件