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Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
In Vitro
Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway. Riociguat is metabolized to BAY60-4552 not only via cytochrome P450 isoenzymes 3A4 (CYP3A4), CYP2C8, and CYP2J2, but also via CYP1A1, located in the liver and lungs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK2181236A and BAY 60-4552 provide partial benefit against hypertension-induced end-organ damage. In spontaneously hypertensive stroke-prone rats, a low dose of BAY 60-4552 decreases urine output and improved survival. A high dose also reduces urine output, and in addition reduces microalbuminuria and attenuates the increase in mean arterial pressure. Both the 0.3 and 3 mg/kg/day doses of BAY 60-4552 improves survival of 46 and 69%. Seven weeks of treatment with BAY 60-4552 (0.3 and 3.0 mg/kg/day) dose-dependently decreases urine output to 79±11 and 56±10 mL/day . BAY 60-4552, and vardenafil provides synergistic beneficial effects and might therefore salvage patients who experience treatment failures with PDE5 inhibitors after radical prostatectomy. MCE has not independently confirmed the accuracy of these methods. They are for reference only.