FSL0588

Structure

• InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)
• InChIKey=BOVGTQGAOIONJV-UHFFFAOYSA-N

Synonyms

• 21187-98-4
• Gliclazide

Origin

Chemically synthesized

Biological activities

Insulin secretion

Therapeutic

Antidiabetic

Target

Sulfonylurea receptors (SUR-1)

Assay information

Block of KATP channels in pancreatic beta-cells (IC₅₀ = 184 ± 30 nM), cardiac myocytes (IC₅₀ = 19.5 ± 5.4 μM) and arterial smooth muscle (IC₅₀ = 37.9 ± 1.0 μM) isolated from Mouse
Reduction in the blood glucose level on alloxan induced diabetic Albino Wistar rats fed with pellet contaied 2% gliclazide
Biphasic reduction of blood glucose levels in normal and diabetic rats with maximum activity attained at 2h and 8h, and hypoglycemic activity for rabbits (Max: 4h post dose)
Marked reduction of blood glucose levels in rats/rabbits in combination with aminodarone

References

• Nahar L, Nasrin F, Zahan R, Haque A, Haque E, Mosaddik A
  Comparative study of antidiabetic activity of Cajanus cajan and Tamarindus indica in alloxan-induced diabetic mice with a reference to in vitro antioxidant activity.
  Pharmacognosy Res, 6(2): 180-187 (2014)  24761124  doi: 10.4103/0974-8490.129043
• Lawrence CL, Proks P, Rodrigo GC, Jones P, Hayabuchi Y, Standen NB, Ashcroft FM
  Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells.
  Diabetologia, 44(8): 1019-1025 (2001)  11484080  doi: 10.1007/s001250100595
• Campbell DB, Lavielle R, Nathan C
  The mode of action and clinical pharmacology of gliclazide: a review.
  Diabetes Res Clin Pract, 14 Suppl 2: S21-S36 (1991)  1794262