Guanylate cyclase is an enzyme that catalyzes the formation of guanosine 3',5'-monophosphate (cGMP) from guanosine triphosphate (GTP) and soluble guanylate cyclase (sGC) is the receptor for nitric oxide (NO).1)
1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one (ODQ, 1) is a selective and irreversible inhibitor of sGC2,3) and its inhibition of the enzyme is NO-competitive.4) ODQ decreased the minimum alveolar anesthesia concentration for isoflurane anesthesia in rats but did not affect their arterial blood pressure or heart rate.5)
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Guanylate Cyclase Inhibitor
No.158(July 2013)
References
- 1)Regulation of nitric oxide-sensitive guanylyl cyclase
- 2)Potent and selective inhibition of nitric oxide-sensitive guanylyl cyclase by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
- 3)Novel guanylyl cyclase inhibitor, ODQ reveals role of nitric oxide, but not of cyclic GMP in endothelin-1 secretion
- 4)Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase
- 5)The soluble guanylyl cyclase inhibitor ODQ, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, dose-dependently reduces the threshold for isoflurane anesthesia in rats
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