某些可能的外核苷酸酶抑制剂对豚鼠膀胱中ATP分解及药理作用的影响
The effects of some possible inhibitors of ectonucleotidases on the breakdown and pharmacological effects of ATP in the guinea-pig urinary bladder.
作者信息
Hourani S M, Chown J A
机构信息
Department of Biochemistry, University of Surrey, Guildford, England.
出版信息
Gen Pharmacol. 1989;20(4):413-6. doi: 10.1016/0306-3623(89)90188-2.
PMID:2546853
Abstract
- The effects of some possible inhibitors of ectonucleotidases on the breakdown of extracellular ATP by strips of guinea-pig urinary bladder were investigated. 2. Suramin and ethacrynic acid (10 mM) both inhibited ATP breakdown significantly, and difluorodinitrobenzene (10 mM) inhibited it slightly whereas N-ethylmaleimide, adenosine 5'-(gamma-thiotriphosphate) (ATP-gamma-S) and reactive blue-2 (10 mM) were without effect. 3. The inhibitory effects of suramin on ATP breakdown were non-competitive. 4. Ethacrynic acid (1 mM) irreversibly inhibited contractions of the guinea-pig bladder induced by ATP, substance P, histamine, non-adrenergic, non-cholinergic nerve stimulation or KCl, whereas suramin (100 microM) had no inhibitory effect. 5. The results suggest that suramin might provide a starting point for the design of selective inhibitors of ectonucleotidases.
摘要
- 研究了一些可能的胞外核苷酸酶抑制剂对豚鼠膀胱条带细胞外ATP分解的影响。2. 苏拉明和依他尼酸（10 mM）均显著抑制ATP分解，二氟二硝基苯（10 mM）轻微抑制，而N-乙基马来酰亚胺、腺苷5'-（γ-硫代三磷酸）（ATP-γ-S）和活性蓝-2（10 mM）则无作用。3. 苏拉明对ATP分解的抑制作用是非竞争性的。4. 依他尼酸（1 mM）不可逆地抑制由ATP、P物质、组胺、非肾上腺素能、非胆碱能神经刺激或KCl诱导的豚鼠膀胱收缩，而苏拉明（100 microM）无抑制作用。5. 结果表明，苏拉明可能为设计胞外核苷酸酶选择性抑制剂提供一个起点。
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