Not so EEZE: the 'EDHF' antagonist 14, 15 epoxyeicosa-5(Z)-enoic acid has vasodilator properties in mesenteric arteries

Not so EEZE: the 'EDHF' antagonist 14, 15 epoxyeicosa-5(Z)-enoic acid has vasodilator properties in mesenteric arteries
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DOI:
10.1016/j.ejphar.2004.09.062
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发表时间:
2004-12-15
影响因子:
5
通讯作者:
Mitchell, JA
Mitchell, JA
中科院分区:
医学2区
文献类型:
--
作者:
Harrington, LS;Falck, JR;Mitchell, JA

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P-450代谢物,包括环氧二十碳三烯酸,可能是内皮源性超极化因子(EDHF)的候选者。在本研究中,我们证实了稳定的类似物11-壬氧基-8(Z)-烯酸是一种小鼠血管扩张剂。然而,我们也表明,‘环氧二十碳三烯酸受体’拮抗剂14,15EEZE类似地扩张与U46619、前列腺素F-2pha或甲氧胺收缩的小鼠血管,但不能与内皮素-1或钾收缩。我们认为14,15EEZE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个重要的药理性质,它正越来越多地被用于研究EDHF的性质。(C)2004爱思唯尔B.V保留所有权利。
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 F-2alpha 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. (C) 2004 Elsevier B.V All rights reserved.