Inhibition by mepacrine and p-bromophenacylbromide of phosphoinositide hydrolysis, glucose oxidation, calcium uptake and insulin release in rat pancreatic islets.
Inhibition by mepacrine and p-bromophenacylbromide of phosphoinositide hydrolysis, glucose oxidation, calcium uptake and insulin release in rat pancreatic islets.
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Mepacrine 和对溴苯甲酰溴对大鼠胰岛中磷酸肌醇水解、葡萄糖氧化、钙摄取和胰岛素释放的抑制作用。
DOI：
10.1016/0006-2952(84)90641-5
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发表时间：
1984
影响因子：
5.8
通讯作者：
W. Malaisse
中科院分区：
文献类型：
--
作者：
L. Best;A. Sener;P. Mathias;W. Malaisse
发现Mepacrine和p-溴苯甲酰溴都会损害用3 H-肌醇预先标记的胰岛中响应营养物和激素-神经递质刺激的3 H-肌醇磷酸盐的产生。两种药物还抑制响应葡萄糖或格列本脲的 net45Ca 摄取，并显着改变基础条件和葡萄糖刺激条件下灌注胰岛的 45Ca 和 86Rb 流出模式。此外，胰岛中[U-14C]葡萄糖的氧化会受到mepacrine或对溴苯甲酰溴的损害。研究发现，mepacrine (0.01–1.0 mM) 和对溴苯甲酰溴 (0.03–0.3 mM) 的这些抑制作用均与浓度相关，并且通常伴随着相似程度的胰岛素分泌抑制。这些结果表明，mepacrine 和对溴苯甲酰溴都可以抑制完整胰岛中的磷脂酶 C 活性，但也会损害 45 Ca 和 86 Rb 通量以及营养物质的氧化。这些药物抑制作用的多样性使得它们不适合用于检查特定细胞过程在胰岛功能调节中的作用。
Mepacrine andp-bromophenacylbromide were both found to impair3H-inositol phosphate production in response to both nutrient and hormone-neurotransmitter stimuli in islets prelabelled with3H-inositol. Both drugs also inhibited net45Ca uptake in response to glucose or glibenclamide and considerably modified the patterns of45Ca and86Rb efflux from perifused islets under both basal and glucose-stimulated conditions. In addition, the oxidation of [U-14C] glucose in islets was impaired by either mepacrine orp-bromophenacylbromide. These inhibitory effects were found to be concentration-related for both mepacrine (0.01–1.0 mM) andp-bromophenacylbromide (0.03–0.3 mM) and were accompanied, in general, by a similar degree of inhibition of insulin secretion. These results suggest that both mepacrine andp-bromophenacylbromide can inhibit phospholipase C activity in intact islets, but also impair45Ca and86Rb fluxes and oxidation of nutrients. The diversity of these drugs' inhibitory actions makes them unsuitable tools for examining the role of specific cellular processes in the regulation of islet function.
Mepacrine 和 p-bromophenacyl bromide 对人血小板中花生四烯酸释放的影响。
影响因子：
3.9
作者：
Hofmann,SL;Prescott,SM;Majerus,PW
通讯作者：
Majerus,PW