Rho kinase inhibitor

Vasodilators are a group of dtugs, which relax the smooth muscle cells of the blood vessels and lead to an increased local tissue blood flow, a reduced arterial pressure and a reduced central venous pressure. Vasodilators reduce the cardiac pre-load as well as after-load and thereby reduce cardiac work. They are used in a variety of conditions including hypertension, cardiac failure and treatment/prevention of angina pectoris. Major groups are Ca2+-channel blockers (e.g. dihydropyridines), NO-donators (e.g. organic nitrates), K+-channel openers (minoxidil), phosphodiesterase inhibitors (e.g. sildenafil), Rho-kinase inhibitors (e.g. Y27632) or substances with unknown mechanism of action (e.g. hydralazine). Inhibitors of the... 

Rho kinase inhibitor, Y-27632 Dilates the renal vasculature and inhibits autoregulation in the absence or presence of L-NAME [258]... 

Fasudil is a Rho kinase inhibitor and has been reported to have neuroprotective effects. Administration of fasudil ameliorates spatial learning and memory impairment, attenuates neuronal loss, and neuronal injury induced by Ap 2, and inhibits IL-ip and TNF-a production and NF-kB activation in the rat brain [509-511],... 

Song Y, Chen X, Wang LY, Gao W, Zhu MJ (2013) Rho kinase inhibitor fasudil protects against p-amyloid-induced hippocampal neu-rodegeneration in rats. CNS Neurosci Ther 19 603-610... 

Gojo, A., Utsunomiya, K., Taniguchi, K., Yokota, T., Ishizawa, S., Kanazawa, Y, Kurata, H., and Tajima, N. (2007) The Rho-kinase inhibitor, fasudil, attenuates diabetic nephropathy in streptozotocin-induced diabetic rats. Eur. J. Pharmacol. 568, 242-247. 

Directed differentiation towards retinal lineages has also been investigated for application in cell-based therapies to treat retinopathies and degenerative disorders such as age-related macular dystrophy. The production of retinal cells has recently been reported from ESCs and induced pluripotent stem cells with a cocktail of small molecules in serum-free conditions an ALK inhibitor, a Rho kinase inhibitor and a casein kinase inhibitor. ... 

Furuya, T, Hashimoto, M, Koda, M, Okawa, A, Murata, A, Takahashi, K, Yamashita, T, and Yamazaki, M. 2009. Treatment of rat spinal cord injury with a Rho-kinase inhibitor and bone marrow stromal cell transplantation. Brain Res 1295 192-202. 

Schroter, T. et al. 2008. Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II). J. Biomol. Screen. 13, 17-28. 

Y-27632 (25) is a synthetic pyridine derivative that inhibits Rho kinase (ROCK)-I and ROCK-II. As expected, Y27632 (25) inhibits the formation of stress fibers in cultured cells and motility in a number of systems [36]. In addition, two isoquinoline sulfonamides, HA1077 (26) and H-1152 (27), were developed as ROCK inhibitors [37,38]. 

We have shown that Cdc24, the activator of the Rho G-pro-tein Cdc42, is necessary for chemotropism during yeast mating (3). Two other proteins, the heterotrimeric G-protein (7-9) and the cyclin-dependent kinase inhibitor Farl (2, 5), are similarly required... 

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