激动剂能够区分克隆的人源和鼠源前列环素受体。
Agonists can discriminate between cloned human and mouse prostacyclin receptors.
作者信息
Chow K B S, Jones R L, Wise H
机构信息
Department of Pharmacology, Faculty of Medicine, Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.
出版信息
Prostaglandins Leukot Essent Fatty Acids. 2004 May;70(5):423-9. doi: 10.1016/j.plefa.2003.08.022.
The ability of prostacyclin analogues to stimulate adenylyl cyclase (AC) and phospholipase C (PLC) in Chinese hamster ovary (CHO) cells expressing cloned human (hIP) or cloned mouse (mIP) prostacyclin receptors has been compared. For hIP, the order of potency (pEC(50)) for stimulating AC and PLC pathways was similar: AFP-07 (9.3, 8.4)>cicaprost (8.3, 6.9), iloprost (7.9, 6.8)>taprostene (7.4, 6.8)>carbacyclin (6.9, 6.6), PGE(1) (6.6, 5.1). Although the standard IP agonists cicaprost and iloprost behaved similarly in both hIP and mIP receptor-expressing cells, carbacyclin and PGE(1) showed significantly higher potency at the mIP receptor, suggesting that the agonist recognition sites on hIP and mIP receptors are not identical. A further distinction between hIP and mIP receptors was found with taprostene, which had greater efficacy at hIP receptors (AC 94%, PLC 14%) than at mIP receptors (AC 77%, PLC 0%) (cicaprost=100% in each assay).
已比较了前列环素类似物对表达克隆的人（hIP）或克隆的小鼠（mIP）前列环素受体的中国仓鼠卵巢（CHO）细胞中腺苷酸环化酶（AC）和磷脂酶C（PLC）的刺激能力。对于hIP，刺激AC和PLC途径的效价顺序（pEC(50)）相似：AFP-07（9.3，8.4）>西卡前列素（8.3，6.9），伊洛前列素（7.9，6.8）>他普前列素（7.4，6.8）>卡巴前列素（6.9，6.6），前列腺素E1（PGE(1)）（6.6，5.1）。尽管标准的IP激动剂西卡前列素和伊洛前列素在表达hIP和mIP受体的细胞中的表现相似，但卡巴前列素和PGE(1)在mIP受体上的效价显著更高，这表明hIP和mIP受体上的激动剂识别位点并不相同。他普前列素在hIP和mIP受体之间还有进一步的区别，其在hIP受体（AC 94%，PLC 14%）上的效力高于mIP受体（AC 77%，PLC 0%）（每种测定中西卡前列素=100%）。
Zotero 插件