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Gliclazide

CAS No:
21187-98-4 Categories: , ,
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Product Details:

  • Product Name: Gliclazide
  • CAS #: 21187-98-4
  • Mode of Action:

    Gliclazide binds to the _ cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the _ cells. This opens voltage-dependent calcium channels in the _ cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

  • Pharmacodynamics:

    Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates _ cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.

  • Metabolism:

    Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.

  • Toxicity:

    LD50=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.

  • IUPAC: 1-[(4-methylbenzene)sulfonyl]-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea
  • ATC: A10BB09
  • PubChem: 3475
  • DrugBank: DB01120 (APRD00460)
  • Formula: C27H33N3O6S
  • Molecular Mass: 323.411
  • Synonyms: 1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea 1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea Gliclazida [INN-Spanish] Gliclazidum [INN-Latin] N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea
  • SMILES: CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN1CC2CCCC2C1
  • AHFS Code: 08:20.2
  • InChl: BOVGTQGAOIONJV-UHFFFAOYSA-N
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