生物活性 | |||
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描述 | NPPB is a blocker of the outwardly rectifying chloride channel (ORCC). Dose-dependent inhibition of chloride currents is observed with a 50% inhibitory concentration (IC50) of 125 μM NPPB. NPPB itself also shows cytotoxicity against glioma cells with a GI50 of approximately 500 μM. TMZ(Temozolomide)-NPPB blocked chloride currents in U373MG, a severely invasive human glioma cell line, and suppressed migration and invasion of U373MG cells[1]. NPPB treatment inhibited proliferation, migration, cell cycle progression and synthesis of the ECM(extracellular matrix), while promoting apoptosis in HConFs(human conjunctival fibroblasts), by inhibiting the PI3K̸AKT(phosphoinositide 3-kinase/protein kinase B) signaling pathway[2]. NPPB triggered Ca(2+) efflux from mature zone of tea root and significantly increased relative CaM in tea roots. Besides, pretreatment with the Ca(2+) chelator (EGTA) and CaM antagonists (CPZ and TFP) suppressed NPPB-elevated cytosolic Ca(2+) fluorescence intensity and CaM concentration in tea roots, respectively[3]. NPPB could significantly prevent the formation of peritoneal adhesion in rats and inhibit the proliferation of AFB in a concentration-dependent manner. NPPB also reduced the migration of AFB (adhesion fibroblasts) cells with an IC50 of 53.09 μM. Moreover, 100 μM NPPB almost completely eliminated the capacity of regulatory volume decrease (RVD) in these cells[4]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01355380 | - | Completed | - | Poland ... 展开 >> Many Locations, Poland 收起 << | |
NCT00586027 | - | Completed | - | Germany ... 展开 >> Klinikum der Stadt Ludwigshafen, Department of Anesthesiology and Intensive Care Medicine Ludwigshafen, Germany, 67063 收起 << | |
NCT02792452 | - | Recruiting | July 2018 | United Kingdom ... 展开 >> Northwick Park Hospital Recruiting Harrow, MIddx, United Kingdom, HA1 3UJ Contact: Anastasia Vamvakidou 0208 869 2547 anastasia.vamvakidou@nhs.net Contact: Ann Banfield 0208 869 2547 annbanfield@nhs.net 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.33mL 0.67mL 0.33mL |
16.65mL 3.33mL 1.66mL |
33.30mL 6.66mL 3.33mL |
参考文献 |
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