Hydroxyfasudil, a ROCK inhibitor, shows IC50 values of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. It less potently inhibits PKA with an IC50 of 37 μM. Hydroxyfasudil enhances eNOS mRNA levels (EC50 of 0.8 ± 0.3 μM), and between 0-100 μM, it increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). At 10 μM, it prolongs the half-life of eNOS mRNA from 13 to 16 hours without affecting eNOS promoter activity [1].
体内研究
Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both average and maximal voided volumes and reduces maximal detrusor pressure in SD rats [2].
Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs), and at doses of 3 and 10 mg/kg, it significantly improves decreased penile cGMP levels in these rats [3].
体外研究
Hydroxyfasudil, a ROCK inhibitor, shows IC50 values of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. It less potently inhibits PKA with an IC50 of 37 μM. Hydroxyfasudil enhances eNOS mRNA levels (EC50 of 0.8 ± 0.3 μM), and between 0-100 μM, it increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). At 10 μM, it prolongs the half-life of eNOS mRNA from 13 to 16 hours without affecting eNOS promoter activity [1].
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