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BRENDA support

Literature summary for 4.6.1.2 extracted from

  • Kollau, A.; Opelt, M.; Woelkart, G.; Gorren, A.C.F.; Russwurm, M.; Koesling, D.; Mayer, B.; Schrammel, A.
    Irreversible activation and stabilization of soluble guanylate cyclase by the protoporphyrin IX mimetic cinaciguat (2018), Mol. Pharmacol., 93, 73-78 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
cinaciguat cinaciguat activates the heme-free enzyme in a concentration-dependent manner with an EC50 value of about 0.2 microM and maximal cGMP formation at 10 microM. The compound causes time- and concentration-dependent relaxation of precontracted vessels with a maximal effect observed at 90 minutes. The dilatory response is not affected by extensive washout of the drug. Cinaciguat-induced vasodilation is associated with a time- and concentration-dependent increase of cGMP levels. The effect of cinaciguat on 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one-oxidized (ferric) soluble guanylate cyclase is moderate, reaching about 10%-15% of maximal activity Sus scrofa

Organism

Organism UniProt Comment Textmining
Sus scrofa
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Source Tissue

Source Tissue Comment Organism Textmining
artery coronary artery Sus scrofa
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