Oldershaw K A, Taylor C W
Department of Pharmacology, Cambridge, UK.
FEBS Lett. 1990 Nov 12;274(1-2):214-6. doi: 10.1016/0014-5793(90)81366-v.
In permeabilized rat hepatocytes a maximal concentration (25 microM) of 2,5-di-(tert-butyl)-1,4-benzohydroquineone (tBuBHQ) mobilized 70% of sequestere Ca2+ and a half-maximal effect was produced by 1.7 microM tBuBHQ. Inositol 1,4,5-trisphosphate (Ins(1,4,5)P3) stimulated release of about 40% of the intracellular Ca2+ stores. Combined applications of a range of tBuBHQ concentrations with a maximal concentration of Ins(1,4,5)P3 demonstrated that tBuBHQ has slight selectivity for the Ca2+ transport process of the Ins(1,4,5)P3-sensitive stores. We conclude that the Ins(1,4,5)P3-sensitive stores are a subset of those sensitive to tBuBHQ and that the latter is therefore unlikely to prove useful as a tool to discriminate Ins(1,4,5)P3-sensitive and -insensitive Ca2+ stores though it may provide opportunities to design more selective agents.
在通透的大鼠肝细胞中,2,5-二(叔丁基)-1,4-苯并氢醌(tBuBHQ)的最大浓度(25微摩尔)可动员70%的螯合钙,1.7微摩尔的tBuBHQ产生半数最大效应。肌醇1,4,5-三磷酸(Ins(1,4,5)P3)刺激释放约40%的细胞内钙储存。一系列tBuBHQ浓度与最大浓度的Ins(1,4,5)P3联合应用表明,tBuBHQ对Ins(1,4,5)P3敏感储存的钙转运过程具有轻微选择性。我们得出结论,Ins(1,4,5)P3敏感储存是对tBuBHQ敏感的储存的一个子集,因此,尽管tBuBHQ可能为设计更具选择性的药物提供机会,但它不太可能作为区分Ins(1,4,5)P3敏感和不敏感钙储存的工具。