毒理性
AZ-4在静息细胞中并未改变细胞质Ca2+。然而,该毒素以剂量依赖性方式抑制了由毛茛素(Tg)诱导的细胞质Ca2+水平的增加。AZ-4降低了由Tg引起的Ca2+内流,但并未影响由该药物引起的内储Ca2+的释放。AZ-4对Tg诱导的Ca2+内流的影响是可逆的,并不受环磷酸腺苷(cAMP)途径的调节。当AZ-4在镍之前、之后或与其同时加入时,作为Ca2+通道的非特异性阻断剂,其效果无法区分且是叠加的。AZ-4还抑制了鸡冠素(MTX)刺激的Ca2+内流约5至10%。
... AZ-4 did not modify cytosolic Ca2+ in resting cells. However, the toxin dose-dependent inhibited the increase in cytosolic Ca2+ levels induced by thapsigargin (Tg). AZ-4 decreased Ca2+-influx induced by Tg but did not affect the Ca2+-release from internal stores induced by this drug. The effects of AZ-4 on Ca2+-influx induced by Tg were reversible and not regulated by adenosine 3',5'-cyclic monophosphate (cAMP) pathway. When AZ-4 was added before, after or together with nickel, an unspecific blocker of Ca2+ channels, the effects were indistinguishable and additive. AZ-4 also inhibited maitotoxin (MTX)-stimulated Ca2+-influx by 5 to 10%.
来源:Hazardous Substances Data Bank (HSDB)