Adeagbo A S, Malik K U
Department of Pharmacology, College of Medicine, University of Tennessee, Memphis.
J Pharmacol Exp Ther. 1991 Aug;258(2):452-8.
The contribution of K+ channels and cytochrome P450 generated arachidonic acid (AA) metabolites to the endothelium-dependent vasodilation produced by this fatty acid in the perfused rat isolated mesenteric arteries was examined using a variety of compounds known to inhibit transmembrane K+ channels and cytochrome P450 enzymes. AA (1-1000 nmol) caused dose- and endothelium-dependent vasodilation in the presence of indomethacin and the effect was neither altered by lipoxygenase (AA 861) nor cytochrome P450 monooxygenase (alpha-naphthoflavone, ketoconazole and metyrapone) inhibitors indicating that AA-induced, endothelium-dependent vasodilation in this vascular bed was not mediated by product(s) of AA metabolism. The vasodilator effect of AA was also not altered by L-NG-nitro-arginine, methylene blue (50 microM), oxyhemoglobin (5 microM) or superoxide dismutase (50 U/ml), thus ruling out nitric oxide being its mediator. Conversely, arterial perfusion with K(+)-free or excess (50 mM) K+ Krebs' solution, but not ouabain infusion, minimized the vasodilator effect of AA, suggesting that this action of the fatty acid is due to changes in membrane K+ conductance that is independent of Na+/K(+)-adenosine triphosphatase activity. The vasodilator action of BRL 34915 (a K+ channel activator) was also minimized by extracellular K+ depletion or excess K+ (50 mM), but not by ouabain. Apamin (0.5 microM) and crude scorpion venom (2.5 micrograms/ml) attenuated AA- but not BRL 34915-induced vasodilation. Glyburide (inhibitor of ATP-activated K+ channel) abolished the vasodilator action of AA and BRL 34915. Procaine, a nonspecific K+ channel blocker did not affect AA-induced vasodilation even though it attenuated that caused by BRL 34915.(ABSTRACT TRUNCATED AT 250 WORDS)
利用多种已知可抑制跨膜钾通道和细胞色素P450酶的化合物,研究了钾通道和细胞色素P450生成的花生四烯酸(AA)代谢产物对该脂肪酸在灌注大鼠离体肠系膜动脉中产生的内皮依赖性血管舒张的作用。在吲哚美辛存在的情况下,AA(1 - 1000 nmol)引起剂量和内皮依赖性血管舒张,且该效应既不受脂氧合酶(AA 861)抑制剂影响,也不受细胞色素P450单加氧酶(α - 萘黄酮、酮康唑和甲吡酮)抑制剂影响,这表明在该血管床中AA诱导的内皮依赖性血管舒张不是由AA代谢产物介导的。AA的血管舒张作用也不受L - NG - 硝基精氨酸、亚甲蓝(50 microM)、氧合血红蛋白(5 microM)或超氧化物歧化酶(50 U/ml)影响,因此排除了一氧化氮作为其介质。相反,用无钾或过量(50 mM)钾的克雷布斯溶液灌注动脉,但不是哇巴因输注,可使AA的血管舒张作用最小化,这表明该脂肪酸的这一作用是由于膜钾电导的变化,且与钠/钾 - 腺苷三磷酸酶活性无关。BRL 34915(一种钾通道激活剂)的血管舒张作用也因细胞外钾耗竭或过量钾(50 mM)而最小化,但不受哇巴因影响。蜂毒明肽(0.5 microM)和粗蝎毒(2.5微克/毫升)减弱了AA诱导的血管舒张,但不影响BRL 34915诱导的血管舒张。格列本脲(ATP激活钾通道抑制剂)消除了AA和BRL 34915的血管舒张作用。普鲁卡因,一种非特异性钾通道阻滞剂,即使减弱了BRL 34915引起的血管舒张,也不影响AA诱导的血管舒张。(摘要截短于250字)