Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).

ROCK2:0.72 μM, ROCK1:0.73 μM

Hydroxyfasudil 对 PKA 的抑制作用较弱（IC50: 37 μM），是 ROCKs 的抑制作用的50倍。此外，Hydroxyfasudil 能增加 eNOS mRNA 的水平（EC50: 0.8 ± 0.3 μM），并且以浓度依赖的方式（0-100 μM）提高 eNOS 活性，刺激 NO 在 HAEC 中的产生。Hydroxyfasudil（10 μM）能将 eNOS mRNA 的半衰期从13小时增加到16小时，但对 eNOS 启动子活性（0.1-100 μM）无影响。

Hydroxyfasudil（10 mg/kg，i.p.）在SD大鼠中显著增加了最大和平均排尿量。Hydroxyfasudil还显著降低了膀胱逼尿肌的最大压力。在自发性高血压大鼠（SHRs）中，Hydroxyfasudil（3 mg/kg，i.p.）抑制了由去甲肾上腺素引起的超收缩。此外，Hydroxyfasudil（3/10 mg/kg，i.p.）显著改善了大鼠阴茎cGMP含量的减少。

Hydroxyfasudil is formulated in saline.Micturition behavior is studied after administration of either Hydroxyfasudil (10 mg/kg, i.p.) or a corresponding volume of saline. Each rat is placed in a metabolic cage containing a urine collection funnel that is placed over an electronic balance. The balance is connected to a personal computer via a multiport controller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous 24-h period, the computer samples and records the data for the micturition frequency and volumes. The micturition reflex parameters that are collected include: urine volume per micturition, maximal micturition volume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Each monitoring session started at 18.00 hours. Prior to being placed in the metabolic cage at the start of each experimental period, the animals received either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor.