Stout J G, Kirley T L
Department of Pharmacology and Cell Biophysics, College of Medicine, University of Cincinnati, OH 45267-0575, USA.
Biochem Mol Biol Int. 1995 Aug;36(5):927-34.
Several "specific" inhibitors of P2 purinergic receptors (purinoceptors) were evaluated for their ability to inhibit purified chicken gizzard cell membrane ecto-ATPase. The P2 purinoceptor antagonists tested included suramin, triazine based reactive textile dyes, and non-specific total protein dyes. All inhibited the purified ecto-ATPase, with half maximal inhibition from approximately 20 to 120 microM. Thin layer chromatography purified Cibacron Blue 3GA, also known as Reactive Blue 2, was demonstrated to inhibit immunopure ecto-ATPase with an IC50 of 44 microM. Thus, for the first time, these compounds used to pharmacologically classify the subtypes of P2 purinoceptors are demonstrated to have direct inhibitory effects on purified ecto-ATPase. Therefore, data generated using these compounds on purinoceptors must be interpreted in light of their direct inhibitory effect on the ecto-ATPase found in the same tissues.
对几种P2嘌呤能受体（嘌呤受体）的“特异性”抑制剂抑制纯化鸡砂囊细胞膜外ATP酶的能力进行了评估。所测试的P2嘌呤受体拮抗剂包括苏拉明、基于三嗪的活性纺织染料和非特异性总蛋白染料。所有这些都抑制了纯化的外ATP酶，半数最大抑制浓度约为20至120微摩尔。经薄层色谱纯化的汽巴克隆蓝3GA（也称为活性蓝2）被证明能抑制免疫纯外ATP酶，其半数抑制浓度为44微摩尔。因此，首次证明这些用于从药理学上对P2嘌呤受体亚型进行分类的化合物对纯化的外ATP酶具有直接抑制作用。因此，使用这些化合物在嘌呤受体上产生的数据必须根据它们对同一组织中外ATP酶的直接抑制作用来进行解释。
