Title of article
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides
Author/Authors
Christopher Fotsch، نويسنده , , Nianhe Han، نويسنده , , Premilla Arasasingham، نويسنده , , Yunxin Bo، نويسنده , , Michelle Carmouche، نويسنده , , Ning Chen، نويسنده , , James Davis، نويسنده , , Martin H. Goldberg، نويسنده , , Clarence Hale، نويسنده , , Feng-Yin Hsieh، نويسنده , , Michael G. Kelly، نويسنده , , Qingyian Liu، نويسنده , , Mark H. Norman، نويسنده , , Duncan M. Smith، نويسنده , , Markian Stec، نويسنده , , Nuria Tamayo، نويسنده , , Ning Xi، نويسنده , , Shimin Xu، نويسنده , , Anthony W. Bannon، نويسنده , , James W. Baumgartner، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
1623
To page
1627
Abstract
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.
Keywords
piperazine , Melanocortin subtype 4 receptor , feeding
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795448
Link To Document