Sovesudil (PHP-201) hydrochloride 是一种有效的、ATP 竞争性局部作用 Rho 激酶 (ROCK) 抑制剂，对 ROCK I 和 ROCK II 的 IC50 分别为 3.7和2.3 nM。Sovesudil hydrochloride 可降低眼压而不引起充血。
Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia[1][2].
Sovesudil (PHP-201) (1 μM; 60 min) hydrochloride is able to induce altered cellular behavior of human trabecular meshwork (HTM) cells[1].
Sovesudil (0.1%, 0.3%, and 0.5%; male New Zealand White rabbits) hydrochloride effectively reduces Intraocular Pressure (IOP) in ocular normotensive and acute hypertensive rabbits without causing distinct hyperemia[1].
[1]. Van de Velde S, et al. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014;55(2):1006-1016. Published 2014 Feb 18. [2]. Ha A, et al. Sovesudil (locally acting rho kinase inhibitor) for the treatment of normal-tension glaucoma: the randomized phase II study [published online ahead of print, 2021 Jul 28]. Acta Ophthalmol. 2021;10.1111/aos.14949.
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