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HD047703, a New Promising Anti-Diabetic Drug Candidate: In Vivo Preclinical Studies
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  • HD047703, a New Promising Anti-Diabetic Drug Candidate: In Vivo Preclinical Studies
  • HD047703, a New Promising Anti-Diabetic Drug Candidate: In Vivo Preclinical Studies
저자명
Kim. SoRa,Kim. Dae Hoon,Kim. Young-Seok,Ha. Tae-Young,Yang. Jin,Park. Soo Hyun,Jeong. Kwang Won,Rhee. Jae-Keol
간행물명
Biomolecules & therapeutics
권/호정보
2014년|22권 5호|pp.400-405 (6 pages)
발행정보
한국응용약물학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

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 b-cells and intestinal cells. In this study, we identified a novel small-molecule GPR119 agonist, HD047703, which raises intracellular cAMP concentrations in pancreatic ${eta}$-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.