494783-46-9Relevant 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.
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core
Xi, Ning,Hale, Clarence,Kelly, Michael G.,Norman, Mark H.,Stec, Markian,Xu, Shimin,Baumgartner, James W.,Fotsch, Christopher
, p. 377 - 381 (2007/10/03)
A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC50s ranging from 0.1 to 200 nM). Both agonists and antagonists of MC4R were prepared by modi
