Stemazole is a novel small molecule human stem/progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

Stemazole (10, 30, and 100 μM) enhanced clonal expansion from single cells in a dose-dependent fashion and clearly decreased apoptosis from 54.1% to 25.2%. Furthermore, the drug reduced apoptosis from 43.6% to 8.4% over 15 h of starvation, with 66% of astemizole-treated cells remaining viable after 2 weeks of starvation. Importantly, starved cells protected with stemazole retained the same proliferation and differentiation properties as cells in normal culture. Stemazole significantly promotes the survival of stem cells in single-cell or starvation cultures without compromising stemness and pluripotency.[2]

Mice were injected intraperitoneally with MPTP (20mg/kg) four times at 2-h intervals for one day to induce Parkinsonism, and then treated with stemazole (ST) (10, 30 and 50mg/kg) for 7 days. Our results demonstrated that ST treatment improved locomotor activity and motor coordination in MPTP mice. There was also a significant increase in TH-positive cells (∼24%, P<0.01) and DAT levels (∼26%, P<0.01) in MPTP mice treated with ST (50mg/kg) compared with the vehicle group. DA and its metabolite levels were significantly increased with ST (50mg/kg) treatment (P<0.01, compared with the vehicle group). SOD and GSH-PX activities were elevated notably in ST treatment groups compared with the vehicle group. These results suggest that ST has neuroprotective effect on the impaired DA system, potentially through enhancement of the cell's anti-oxidative capacity.[1]