并非如此简单：“内皮衍生超极化因子（EDHF）”拮抗剂14,15-环氧二十碳-5（Z）-烯酸在肠系膜动脉中具有血管舒张特性。
Not so EEZE: the 'EDHF' antagonist 14, 15 epoxyeicosa-5(Z)-enoic acid has vasodilator properties in mesenteric arteries.
作者信息
Harrington Louise S, Falck John R, Mitchell Jane A
机构信息
Unit of Critical Care Medicine, Royal Brompton Hospital, The National Heart and Lung Institute, Imperial College School of Medicine, Dovehouse Street, London, SW3 6LY, UK.
出版信息
Eur J Pharmacol. 2004 Dec 15;506(2):165-8. doi: 10.1016/j.ejphar.2004.09.062.
P-450 metabolites, including the epoxyeicosatrienoic acids, are likely candidates for endothelial derived hyperpolarising factor (EDHF). In the present study, we confirm that the stable analogue 11-nonyloxyundec-8(Z)-enoic acid is a vasodilator of murine vessels. However, we also show that the 'epoxyeicosatrienoic acid receptor' antagonist 14,15 EEZE similarly dilates murine vessels contracted with U46619, prostaglandin F2alpha or methoxamine, but not with endothelin-1 or potassium. We suggest that 14,15 EEZE is a partial agonist for the epoxyeicosatrienoic acids/EDHF receptor. These results illustrate an important pharmacological property of this antagonists, which is being increasingly used to study the nature of EDHF.
包括环氧二十碳三烯酸在内的细胞色素P-450代谢产物很可能是内皮衍生超极化因子（EDHF）的候选物质。在本研究中，我们证实稳定类似物11-壬氧基十一碳-8（Z）-烯酸是小鼠血管的血管舒张剂。然而，我们还表明，“环氧二十碳三烯酸受体”拮抗剂14,15-EEZE同样能舒张由U46619、前列腺素F2α或甲氧明收缩的小鼠血管，但不能舒张由内皮素-1或钾收缩的血管。我们认为14,15-EEZE是环氧二十碳三烯酸/EDHF受体的部分激动剂。这些结果说明了这种拮抗剂的一种重要药理学特性，该拮抗剂正越来越多地用于研究EDHF的性质。
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