Y-39983 Hydrochloride contain Rho kinase inhibitory activity.
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].
In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration[1]. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats[2].
ROCK: 3.6 nM (IC50); PKC: 420 nM (IC50); CaMKII: 810 nM (IC50)
[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.
![(R)-4-(1-aMinoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzaMide dihydrochloride Structure](/CAS/GIF/173897-44-4.gif)
