861102-91-2Relevant articles and documents
2,4-Diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists
Serby, Michael D.,Zhao, Hongyu,Szczepankiewicz, Bruce G.,Kosogof, Christi,Xin, Zhili,Liu, Bo,Liu, Mei,Nelson, Lissa T. J.,Kaszubska, Wiweka,Falls, H. Douglas,Schaefer, Verlyn,Bush, Eugene N.,Shapiro, Robin,Droz, Brian A.,Knourek-Segel, Victoria E.,Fey, Thomas A.,Brune, Michael E.,Beno, David W. A.,Turner, Theresa M.,Collins, Christine A.,Jacobson, Peer B.,Sham, Hing L.,Liu, Gang
, p. 2568 - 2578 (2007/10/03)
Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions with ghrelin antibody, peptidyl GHS-R antagonists, and antisense oligonucleosides resulted in weight loss and food intake decrease in rodents. Here we report the effects of GHS-R antagonists, some of which were potent, selective, and orally bioavailable. A structure-activity relationship study led to the discovery of 8a, which was effective in decreasing food intake and body weight in several acute rat studies.
