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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.
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Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.

机译：丙泊茶碱对转染人A1，A2A或A2B受体和荧光素酶报道基因的中国仓鼠卵巢细胞腺苷受体活性的影响。

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摘要

Propentofylline is neuroprotective in vivo, but its mechanism of action is not completely understood. Previously, propentofylline was shown to block adenosine transport processes, to inhibit three adenosine receptor subtypes, and to inhibit cAMP phosphodiesterase. We tested the effect of propentofylline on adenosine receptor function in Chinese hamster ovary (CHO) cells transfected with human adenosine A1, A2A, or A2B receptors and a luciferase reporter gene under control of a promoter sequence containing several copies of the cAMP response element. We investigated the concentration-dependent inhibitory effects of propentofylline on cAMP phosphodiesterase, adenosine transport processes, and adenosine A1, A2A, and A2B receptors. At concentrations > or = 1 mM, propentofylline increased luciferase activity probably as a result of inhibition of cAMP phosphodiesterase. Inhibition of [3H]adenosine uptake by propentofylline was concentration dependent, with IC50 values of 37-39 microM for the three cell types. Agonist-activated adenosine A1 receptors were antagonized by 100 microM propentofylline, but inhibition of agonist-stimulated A2A or A2B receptors was not observed. In contrast, A1 and A2A receptor mediated effects of adenosine were enhanced by propentofylline at concentrations of 1 and 100 microM, respectively. These data indicate that the net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present.
机译：原戊茶碱在体内具有神经保护作用，但其作用机理尚不完全清楚。以前，propentofylline被证明可以阻止腺苷转运过程，抑制三种腺苷受体亚型，并抑制cAMP磷酸二酯酶。我们测试了丙泊茶碱对转染人腺苷A1，A2A或A2B受体和荧光素酶报告基因的中国仓鼠卵巢（CHO）细胞中腺苷受体功能的影响，该启动子序列包含多个cAMP反应元件的启动子序列。我们研究了丙泊茶碱对cAMP磷酸二酯酶，腺苷转运过程以及腺苷A1，A2A和A2B受体的浓度依赖性抑制作用。在浓度大于或等于1 mM时，丙氧茶碱可能增加了萤光素酶的活性，这可能是由于抑制了cAMP磷酸二酯酶的结果。丙泊茶碱对[3H]腺苷摄取的抑制是浓度依赖性的，三种细胞类型的IC50值为37-39 microM。激动剂激活的腺苷A1受体被100 microM丙氧茶碱拮抗，但未观察到激动剂刺激的A2A或A2B受体的抑制作用。相反，丙戊茶碱在1和100 microM的浓度下分别增强A1和A2A受体介导的腺苷作用。这些数据表明，丙泊茶碱在体内的净作用将取决于可用的丙泊茶碱和腺苷的浓度以及存在的腺苷受体，磷酸二酯酶和核苷转运蛋白的亚型。

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