Background:

Y-39983 dihydrochloride is a novel and selective inhibitor of ROCK family with IC50 value of 3.6nM for ROCK [1].

Y-39983 dihydrochloride has shown a selective inhibitor of Rho-associated coiled coil-forming protein kinase( ROCK ) with IC50 values of 3.6nM, 0.42μM and 0.81μM for ROCK, PKC and CaMKII, respectively [1]. Apart from these, Y-39983 has been reported to relax the ciliary arteries of precontracted isolated rabbit in vitro. In addition, Y-39983 has been found to increase optic-nerve-head blood flow by laser speckle flowmetry [2]. Moreover, Y-39983 lowered the intraocular pressure ( IOP) in a dose-dependent fashion in the eyes of rabbits and monkeys [1].

参考文献:
[1] Tokushige H1, Inatani M, Nemoto S, Sakaki H, Katayama K, Uehata M, Tanihara H. Effects of topical administration of y-39983, a selective rho-associated protein kinase inhibitor, on ocular tissues in rabbits and monkeys. Invest Ophthalmol Vis Sci. 2007 Jul;48(7):3216-22.
[2] Watabe H1, Abe S, Yoshitomi T. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries. Jpn J Ophthalmol. 2011 Jul;55(4):411-7. doi: 10.1007/s10384-011-0048-9. Epub 2011 Jun 11.