Imeglimin lowers glucose primarily by amplifying glucose-stimulated insulin secretion in high-fat-fed rodents
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Imeglimin is a promising new oral antihyperglycemic agent that has been studied in clinical trials as a possible monotherapy or add-on therapy to lower fasting plasma glucose and improve hemoglobin A1c (1-3, 9). Imeglimin was shown to improve both fasting and postprandial glycemia and to increase insulin secretion in response to glucose during a hyperglycemic clamp after 1-wk of treatment in type 2 diabetic patients. However, whether the β-cell stimulatory effect of imeglimin is solely or partially responsible for its effects on glycemia remains to be fully confirmed. Here, we show that imeglimin directly activates β-cell insulin secretion in awake rodents without affecting hepatic insulin sensitivity, body composition, or energy expenditure. These data identify a primary amplification rather than trigger the β-cell mechanism that explains the acute, antidiabetic activity of imeglimin.
Original language | English |
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Journal | American Journal of Physiology: Endocrinology and Metabolism |
Volume | 311 |
Issue number | 2 |
Pages (from-to) | E461-70 |
ISSN | 0193-1849 |
DOIs | |
Publication status | Published - 1 Aug 2016 |
- Animals, Blood Glucose, Diet, High-Fat, Fasting, Glucose, Glucose Clamp Technique, Hypoglycemic Agents, Insulin, Insulin Resistance, Insulin-Secreting Cells, Liver, Male, Mice, Mice, Inbred C57BL, Postprandial Period, Rats, Rats, Sprague-Dawley, Triazines, Journal Article
Research areas
ID: 180401936