Chakravarty N
Acta Pharmacol Toxicol (Copenh). 1980 Sep;47(3):223-35. doi: 10.1111/j.1600-0773.1980.tb01564.x.
The role of a Ca++-MG++ activated ATPase, demonstrated on the outer surface of rat peritoneal mast cells, on histamine release induced by antigen (anaphylactic reaction), compound 48/80 and ionophore A23187 has been studied. A high level of the enzyme activity is retained at the optimal pH for histamine release induced by the three releasing agents. The effect of fourteen inhibitors of ATPase has been studied, viz. quinidine, fluoride, platinum salt, suramin, ethacrynic acid, ethyl alcohol, N-ethylmaleimide, Mn++, Ni++, ADP, AMP and the flavones: kaempferol, quercetin, morin. All the inhibitors, which caused varying degrees of inhibition of ATPase, also inhibited histamine release. The inhibition of the enzyme was competitive with ADP, AMP, ethacrynic acid, suramin and morin and non-competitive with the others. The degree of inhibition of ATPase and of histamine release tended to be similar with six inhibitors. With the others the extent of the inhibition of the release and of the enzyme varied. But a marked inhibition of the enzyme was always associated with a pronounced inhibition of histamine release. ATP in lower concentrations (10-20 microM) has been shown to potentiate histamine release induced by all the three releasers, possibly through its utilization by plasma membrane ATPase. The observations agree with the hypothesis that plasma membrane ATPase participates in the histamine release process.
已对大鼠腹膜肥大细胞外表面上的Ca++-Mg++激活的ATP酶在抗原（过敏反应）、化合物48/80和离子载体A23187诱导的组胺释放中所起的作用进行了研究。在由这三种释放剂诱导组胺释放的最佳pH条件下，该酶活性保持在较高水平。已研究了14种ATP酶抑制剂的作用，即奎尼丁、氟化物、铂盐、苏拉明、依他尼酸、乙醇、N-乙基马来酰亚胺、Mn++、Ni++、ADP、AMP以及黄酮类化合物：山奈酚、槲皮素、桑色素。所有这些引起不同程度ATP酶抑制的抑制剂也都抑制组胺释放。该酶的抑制作用与ADP、AMP、依他尼酸、苏拉明和桑色素呈竞争性，与其他抑制剂呈非竞争性。六种抑制剂对ATP酶和组胺释放的抑制程度趋于相似。对于其他抑制剂，释放和酶的抑制程度各不相同。但酶的明显抑制总是与组胺释放的显著抑制相关。较低浓度（10-20 microM）的ATP已被证明可增强由所有三种释放剂诱导的组胺释放，这可能是通过质膜ATP酶对其的利用实现的。这些观察结果与质膜ATP酶参与组胺释放过程的假说相符。
