Y-27632 dihydrochloride,129830-38-2,IC-0242294

Y-27632 dihydrochloride, as a selective Rho-kinase inhibitor, is a novel bronchodilator.[1]

In vitro, treatment with 3 and 10 μM Y-27632 remarkably reduced the maximal contractile response. And Y-27632 (10 μM ) markedly increased the EFS-induced outflow of radioactivity from airway cholinergic nerves by 27% and 54% respectively, in murine and guinea-pig tracheal preparations loaded with [(3)H]-choline.[2] In vitro, Y-27632 at 10 μM abolished stress fibers in Swiss 3T3 cells, but it had no effect in the G(1)-S phase transition of the cell cycle and cytokinesis.[3] In vitro, treatment with 10 μM Y-27632 and hypoxia further increased the expression of ACAN and COL2A1 in chondrocytic cells.[4] In vitro, 100 μM Y-27632 significantly promoted cell proliferation and phagocytosis of trabecular meshwork cells.[6]

In vivo efficacy test it shown that Y-27632 inhalation (1 mM, 2 min) inhibited acetylcholine- or ovalbumin-induced increase in R(L) and had no changes in mean blood pressure, and the effect last for at least 3 h.[1] In vivo experiment it indicated that injection 5mg/kg Y-27632 intravenously markedly decreased the serum levels of interleukin-6 (IL-6), IL-1β, tumor necrosis factor-α (TNF-α) and increased IL-10 level in serum of MRL/lpr mice.[5] In addition, treatment with 2 or 30 mg/kg body weight of Y-27632 orally in SOD1(G93A) mice, Y-27632 improved motor function in male mice at 30 mg/kg, but it had no benefit at 2 mg/kg.[7]