- 生物活性
Fluspirilene是L型钙通道的非竞争性拮抗剂,IC50为0.03 μM。Fluspirileneis是一种用于精神分裂症的长效可注射抗精神病药物。
- 靶点
IC50: 0.03 μM (L-type calcium channel)
- 体外研究
Fluspirilene, at concentrations which non-competitively modify dihydropyridine binding, selectively antagonizes the effects of calcium-channel activators. Fluspirilene decreases the viability and suppresses sphere-forming of glioma stem cell lines in a dose-dependent manner. Fluspirilene demonstrates the inhibition of proliferation of T98, U87 and all GSC lines at 1.25, 2.5, and 5 μM, while it inhibits the proliferation of U251 and SNB19 at 2.5 and 5 μM.
- 体内研究
Mice treated with fluspirilene shows a remarkable reduction of the tumor size. Fluspirilene significantly prolongs survival of the TGS04 mouse model.