Inhibition of rat parotid ecto-ATPase activity
Inhibition of rat parotid ecto-ATPase activity
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DOI：
10.1016/s0003-9969(99)00100-4
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发表时间：
1999-12-01
影响因子：
3
通讯作者：
Zeng, W
中科院分区：
文献类型：
--
作者：
Dowd, FJ;Li, LS;Zeng, W
比较了几种已知和可疑的外膜ATP酶抑制剂对大鼠腮腺质膜外膜ATP酶活性的抑制作用。具有高IC 50（高于130 μ M）的那些化学物质是核苷酸α，β-亚甲基ATP、β，γ-亚甲基ATP、2-甲硫基ATP、肌苷三磷酸。5 ′-对氟磺酰基苯甲酰腺苷、磺酸盐、1-氨基-2-萘酚-4-磺酸、考马斯亮蓝G.和二苯乙烯二磺酸盐，DIDS和SITS。具有低IC 50的那些药剂是：考马斯亮蓝R（114 μ M）、ATP γ S（49 μ M）、苏拉明（72 μ M）和活性蓝2（25 μ M）。最后三种抑制剂与整个腮腺腺泡细胞的ATP水解抑制剂具有相似的效力。ARL 67156是一种选择性的胞外ATP酶抑制剂，其IC 50约为100。一百二十亩苏拉明显示非竞争性抑制外ATP酶，而ATP γ S和活性蓝2的抑制作用的狄克逊图曲线。这些结果定义了各种试剂对外分泌组织中的外-ATP酶的影响，所述外分泌组织已被证明对细胞外ATP有反应。(C)1999 Elsevier Science Ltd.保留所有权利。
The inhibitory profile of several known and suspected ecto-ATPase inhibitors was compared on ecto-ATPase activity in rat parotid plasma membranes. Those chemicals with high IC50 (above 130 mu M) were the nucleotides alpha,beta-methylene ATP, beta,gamma-methylene ATP, 2-methylthio ATP, inosine triphosphate. 5'-p-fluorosulphonylbenzoyladenosine, the sulphonates, 1-amino-2-naphthol-4-sulphonic acid, Coomassie brilliant blue G. and the stilbene disulphonates, DIDS and SITS. Those agents with low IC50 were: Coomassie brilliant blue R (114 mu M), ATP gamma S (49 mu M), suramin (72 mu M) and Reactive blue 2 (25 mu M). The last three inhibitors have similar potencies as inhibitors of ATP hydrolysis by whole parotid acinar cells. ARL67156, a selective inhibitor of ecto-ATPase, had an IC50 of approx. 120 mu M. Suramin displayed non-competitive inhibition of ecto-ATPase whereas the inhibitory effects of ATP gamma S and Reactive blue 2 were curvilinear on Dixon plots. These results define the effects of various agents on ecto-ATPase in an exocrine tissue that has been shown to respond to extracellular ATP. (C) 1999 Elsevier Science Ltd. All rights reserved.