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Description

Fasudil is a rho-associated kinase (ROCK) inhibitor that exhibits cardioprotective, vasodilatory, neuroprotective, anti-inflammatory, and anti-angiogenic activities. In animal models of myocardial ischemia/reperfusion, fasudil increases expression of Bcl-2 and p-Akt and decreases expression of Bax and caspase 3, decreasing myocardial infarction size. In other heart failure models, fasudil decreases activation of JNK, translocation of ERK, and expression of c-fos and c-jun. Fasudil also decreases activity of matrix metalloproteinase 9 (MMP9). This compound decreases aneurysm size in models of abdominal aortic aneurysm and also inhibits progression of existing aneurysms in vivo. In animal models of amyotrophic lateral sclerosis (ALS), fasudil decreases motor neuron loss, slowing disease progression and increasing survival time. In animal models of experimental autoimmune encephalitis (EAE), this compound decreases production of toll-like receptor 4 (TLR4), NF-κB, IL-1β, IL-6, and TNF-α and increases production of IL-10 and cannabinoid receptor 2 (CBR2). Additionally, fasudil decreases expression of fibrotic mediators and upregulates expression of prolyl hydroxylase 2, downregulating expression of HIF-1α in diabetic mice.

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References

Peng C, Gu P, Zhou J, et al. Inhibition of rho-kinase by fasudil suppresses formation and progression of experimental abdominal aortic aneurysms. PLoS One. 2013 Nov 14;8(11):e80145. PMID: 24244631.

Takata M, Tanaka H, Kimura M, et al. Fasudil, a rho kinase inhibitor, limits motor neuron loss in experimental models of amyotrophic lateral sclerosis. Br J Pharmacol. 2013 Sep;170(2):341-51.PMID: 23763343.

Matoba K, Kawanami D, Okada R, et al. Rho-kinase inhibition prevents the progression of diabetic nephropathy by downregulating hypoxia-inducible factor 1α. Kidney Int. 2013 Sep;84(3):545-54. PMID: 23615507.

Jiang ZH, Zhang TT, Zhang JF. Protective effects of fasudil hydrochloride post-conditioning on acute myocardial ischemia/reperfusion injury in rats. Cardiol J. 2013;20(2):197-202. PMID: 23558879.

Hou SW, Liu CY, Li YH, et al. Fasudil ameliorates disease progression in experimental autoimmune encephalomyelitis, acting possibly through antiinflammatory effect. CNS Neurosci Ther. 2012 Nov;18(11):909-17. PMID: 22994384.

Ishiguro M, Kawasaki K, Suzuki Y, et al. A Rho kinase (ROCK) inhibitor, fasudil, prevents matrix metalloproteinase-9-related hemorrhagic transformation in mice treated with tissue plasminogen activator. Neuroscience. 2012 Sep 18;220:302-12. PMID: 22710066.

Raja SG. Evaluation of clinical efficacy of fasudil for the treatment of pulmonary arterial hypertension. Recent Pat Cardiovasc Drug Discov. 2012 Aug;7(2):100-4. PMID: 22670803.

Wang N, Guan P, Zhang JP, et al. Fasudil hydrochloride hydrate, a Rho-kinase inhibitor, suppresses isoproterenol-induced heart failure in rats via JNK and ERK1/2 pathways. J Cell Biochem. 2011 Jul;112(7):1920-9. PMID: 21433064.