494782-40-0Relevant academic research and scientific papers
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides
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.
, p. 1623 - 1627 (2007/10/03)
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.
Substituted piperazines and methods of use
-
, (2008/06/13)
Selected substituted piperazine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical com
