关于受体操纵性钙内流阻滞剂SK&F 96365对前列腺素生成的抑制作用
On the inhibition of prostanoid formation by SK&F 96365, a blocker of receptor-operated calcium entry.
作者信息
Leis H J, Zach D, Huber E, Ziermann L, Gleispach H, Windischhofer W
机构信息
Dept. of Biochemical Analysis, Univ. Childrens Hospital, Graz, Austria.
出版信息
Br J Pharmacol. 1995 Feb;114(3):598-601. doi: 10.1111/j.1476-5381.1995.tb17181.x.
Abstract
- The proposed blocker of receptor-operated calcium channels, SK&F 96365 was shown to inhibit formation of prostaglandin E2 in two osteoblast-like cell lines, MC3T3-E1 and UMR-106 in a dose-dependent manner at an IC50 of 3-4 microM. Inhibition was observed with various stimuli (arachidonic acid, bradykinin and calcium ionophore A23187). 2. This effect was also observed in human platelets, where SK&F 96365 dose-dependently blocked thromboxane biosynthesis and formation of 12-hydroxy-heptadecatrienoic acid after stimulation with arachidonic acid (IC50 = 4 microM). 3. The compound had no effect on 12-hydroxy-eicosatetraenoic acid production by human platelets. Additionally, linoleic acid oxidation by soybean 15-lipoxidase was not impaired by SK&F 96365. The results thus provide evidence for cyclo-oxygenase inhibition by SK&F 96365 at concentrations used to block receptor-operated calcium influx.
摘要
- 所提出的受体操纵性钙通道阻滞剂SK&F 96365在两种成骨细胞样细胞系MC3T3-E1和UMR-106中，以剂量依赖方式抑制前列腺素E2的形成，IC50为3 - 4微摩尔。在各种刺激（花生四烯酸、缓激肽和钙离子载体A23187）下均观察到抑制作用。2. 在人血小板中也观察到了这种效应，其中SK&F 96365在用花生四烯酸刺激后剂量依赖性地阻断血栓素生物合成和12-羟基-十七碳三烯酸的形成（IC50 = 4微摩尔）。3. 该化合物对人血小板产生12-羟基-二十碳四烯酸没有影响。此外，SK&F 96365不会损害大豆15-脂氧化酶对亚油酸的氧化作用。因此，这些结果为SK&F 96365在用于阻断受体操纵性钙内流的浓度下抑制环氧化酶提供了证据。
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