Diazoxide

• CAT Number: A000072
• CAS Number: 364-98-7
• Molecular Formula: C8H7ClN2O2S
• Molecular Weight: 230.7
• Purity: ≥95%
• Synonyms: ch-6783, SRG-95213, Proglycem
• Target: AMPAR
• Solubility: >10.4mg/mL in DMSO
• Storage: Store at RT
• IUPAC Name: 7-chloro-3-methyl-4H-1λ6,2,4-benzothiadiazine 1,1-dioxide
• InChI: InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
• InChIKey: GDLBFKVLRPITMI-UHFFFAOYSA-N
• SMILES: CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl

Diazoxide (CAS 364-98-7) is the activator of ATP-dependent K+ channels used for antihypertensive and hyperglycemic activities. Diazoxide increases membrane permeability to potassium ions in vascular smooth muscle, thereby stabilizing the membrane action potential and preventing vascular smooth muscle contraction; this results in peripheral vasodilatation and decreases in peripheral vascular resistance. This agent also inhibits insulin release by interacting with ATP-sensitive potassium channels of pancreatic islet beta-cells.

Overview of Clinical Research

Diazoxide is a potassium channel agonist, which used for antihypertensive and antihypoglycaemics.

Reference

1. Quast et al., /In vitro and in vivo comparison of two K+ channels openers, Diazoxide and Cromakalim, and their inhibition by Glibenclamide./ J. Pharmacol. Exp. Ther. (1989). 250(1):261-271

2. Trube et al., /Opposite effects of Tolbutamide and Diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells./ Pflugers Arch. (1986) 407:493-499

3. Dunne, /Protein phosphorylation is required for Diazoxide to open ATP-sensitive potassium channels in Insulin (RINm5F) secreting cells./ FEBS Lett. (1989). 250(2):262-266

4. Lebrun et al., /Similarities between the effects of Pinacidil and Diazoxide on ionic and secretory events in rat pancreatic islets./ J. Pharmacol. Exp. Ther. (1989). 250:1011

5. Ashford et al., J. Physiol. (1989). 409:53P

6.VIDAL Dictionary, Ed. du Vidal, Paris, (1994). 705