33342-05-1COc1ccc2c(c1)C(=O)N(CCc1ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc1)C(=O)C2(C)CLLJFMFZYVVLQKT-UHFFFAOYSA-N1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-2-isoquinolinyl)ethyl]phenyl]sulfonylurea is a member of isoquinolines.
33342-05-1DTXSID4023096CHEMBL383634CHEBI:93416Pharmaceuticals
Pharmaceuticals -> Listed in ZINC15
2.20e-03 g/L
69.5 [ug/mL] (The mean of the results at pH 7.4)
180-182
181 °C
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A10BB08
A - Alimentary tract and metabolism
QA - Alimentary tract and metabolism
Gliquidone is an anti-diabetic drug in the sulfonylurea class. In patients with diabetes mellitus, there is a deficiency or absence of a hormone manufactured by the pancreas called insulin. Insulin is the main hormone responsible for the control of sugar in the blood. Gliquidone is an antidiabetic medication which is used in those patients with adult maturity onset or non-insulin dependent diabetes (NIDDM). It works by lowering blood sugar levels by stimulating the production and release of insulin from the pancreas. It also promotes the movement of sugar from the blood into the cells in the body which need it.
The mechanism of action of gliquidone in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Gliquidone likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.
개요Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-cells (IC50s = 0.45, 119.1, and 149.7 μM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively). It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay). Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats. It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ; ) when administered at a dose of 10 mg/kg.
용도Gliquidone is an anti diabetic agent used in the treatment of hypoglycemia which leads to an increased risk in diabetic cardiovascular disease. Also used in the treatment diabetic nephropathy.
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