HD047703, a New Promising Anti-Diabetic Drug Candidate: In Vivo Preclinical Studies
- Authors
- Kim, SoRa; Kim, Dae Hoon; Kim, Young-Seok; Ha, Tae-Young; Yang, Jin; Park, Soo Hyun; Jeong, Kwang Won; Rhee, Jae-Keol
- Issue Date
- 30-Sep-2014
- Publisher
- KOREAN SOC APPLIED PHARMACOLOGY
- Keywords
- GPR119 agonist; Type 2 diabetes; GLP-1
- Citation
- BIOMOLECULES & THERAPEUTICS, v.22, no.5, pp.400 - 405
- Journal Title
- BIOMOLECULES & THERAPEUTICS
- Volume
- 22
- Number
- 5
- Start Page
- 400
- End Page
- 405
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/12276
- DOI
- 10.4062/biomolther.2014.035
- ISSN
- 1976-9148
- Abstract
- G-protein coupled receptor 119 (GPR119) has emerged as a novel target for the treatment of type 2 diabetes mellitus. GPR119 is involved in glucose-stimulated insulin secretion (GSIS) from the pancreatic beta-cells and intestinal cells. In this study, we identified a novel small-molecule GPR119 agonist, HD047703, which raises intracellular cAMP concentrations in pancreatic beta-cells and can be expected to potentiate glucose-stimulated insulin secretion from human GPR119 receptor stably expressing cells (CHO cells). We evaluated the acute efficacy of HD047703 by the oral glucose tolerance test (OGTT) in normal C57BL/6J mice. Then, chronic administrations of HD047703 were performed to determine its efficacy in various diabetic rodent models. Single administration of HD047703 caused improved glycemic control during OGTT in a dose-dependent manner in normal mice, and the plasma GLP-1 level was also increased. With respect to chronic efficacy, we observed a decline in blood glucose levels in db/db, ob/ob and DIO mice. These results suggest that HD047703 may be a potentially promising anti-diabetic agent.
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