Description
ODQ (41443-28-1) is a potent and selective inhibitor of soluble guanylyl cyclase (sGC),?IC50?= 20 nM).1 ODQ acts via competition with NO for the heme site of sGC where it binds irreversibly.2?ODQ does not inhibit NO-mediated macrophage toxicity, an activity that is unrelated to cGMP nor does it inhibit particulate GC.1?ODQ is an extremely useful tool to explore the involvement of the NO-cGMP pathway in cellular signaling and physiologic processes.3-5
Chemical Properties
ODQ is off-white to yellow powder
Uses
1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one inhibits neurite outgrowth and causes neurite retraction in PC12 cells independently of soluble guanylyl cyclase.
Uses
ODQ is a selective and potent sGC (soluble guanylyl cyclase) inhibitor.
Definition
ChEBI: 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one is a member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group. It has a role as an EC 4.6.1.2 (guanylate cyclase) inhibitor.
Biological Activity
ODQ is a potent and selective inhibitor of NO-sensitive guanylyl cyclase.
Biochem/physiol Actions
H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) non competitively inhibits the action of nitric oxide-sensitive guanylyl cyclase and results in a supposedly irreversible oxidation of the prosthetic heme group. ODQ has been used to study the role of cyclic guanosine monophosphate (cGMP) pathway in nitric oxide (NO) signal transduction.
References
1) Garthwaite?et al.?(1995),?Potent and Selective Inhibition of Nitric Oxide-sensitive Guanylyl Cyclase by 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one; Mol. Pharmacol.?48?184
2) Schrammel?et al.?(1996),?Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase; Mol. Pharmacol.?50?1
3) Estevez?et al.?(1998),?Nitric oxide-dependent production of cGMP supports the survival of rat embryonic motor neurons cultured with brain-derived neurotrophic factor; J. Neurosci.?18?3708
4) Vandecasteele?et al.?(1998),?Role of the NO-cGMP in the muscarinic regulation of the L-type Ca2+ current in human atrial myocytes; J. Physiol.?506?653
5) Martins-Pinge?et al.?(1999),?Nitric oxide-dependent guanylyl cyclase participates in the glutamatergic neurotransmission within the rostral ventrolateral medulla of awake rats;?Hypertension?34?748
