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Pharmacological characterization and antidiabetic activity of a long‐acting glucagon‐like peptide‐1 analogue conjugated to an antithrombin III ‐binding pentasaccharide
Drug properties and blood sugar-lowering effects of a long-lasting GLP-1 medicine linked to a blood clotting inhibitor
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Abstract
The half-life of the GLP-1 conjugate in mice was ∼11 h.
- In vitro studies showed that insulin secretion from clonal β cells and islets was significantly increased by the GLP-1 conjugate.
- The conjugate demonstrated half maximum effective concentration values of 1.3 × 10(-7) M for GLP-1 receptor binding and 9.9 × 10(-8) M for cAMP generation.
- Significant improvements in blood glucose levels were observed in normal mice following conjugate injection, lasting for over 48 hours.
- Daily treatment of high-fat-fed and ob/ob mice with 25 nmol/kg of the conjugate led to significant enhancements in glucose tolerance and reductions in glycated hemoglobin (HbA1c).
- In db/db mice, treatment with 100 nmol/kg of the conjugate resulted in significant reductions in glucose levels and increases in plasma insulin.
- Islet size and pancreatic insulin content were increased with treatment, while islet cell proliferation and apoptosis remained unchanged.
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