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Biochemical and Biophysical Research Communications 417 (2012) 558–563 Contents lists available at SciVerse ScienceDirect Biochemical and Biophysical Research Communications journal homepage: www.else /loc ate/ybbrc Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently Ye-Hwang Cheong a,b, Mi-Kyung Kim a, Moon-Ho Son a, Bong-Kiun Kaang b,⇑ a Research Center, Dong-A Pharmaceuticals Co. Ltd., 47-5 Sanggal-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-905, Republic of Korea b National Creative Research Initiative Center for Memory, Departments of Biological Sciences and Brain and Cognitive Sciences, College of Natural Sciences, Seoul National University, Seoul 151-747, Republic of Korea a r t i c l e i n f o a b s t r a c t Article history: The glucagon-like peptide-1 receptor (GLP-1R) is a target for type 2 diabetes treatment. Due to the Received 22 November 2011 inconvenience of peptide therapeutics, small-molecule GLP-1R agonists have been studied. Compound Available online 8 December 2011 2 (6,7-dichloro-2-methylsulfonyl-2-N-tert-butylaminoquinoxaline) and compound B (4-(3-(benzyl- oxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine) have been described as small molecule, Keywords: ago-allosteric modulators of GLP-1R. However, their modes of action at the GLP-1R have not been eluci- GLP-1 dated. Thus, in this study, we compared the mechanisms of action between these two compounds. Wh