血小板活化因子（PAF）受体拮抗剂对PAF在大鼠离体灌流心脏中血管舒张和血管收缩作用的不同影响。
Differential actions of platelet-activating factor (PAF) receptor antagonists on the vasodilator and vasoconstrictor effects of PAF in the rat perfused heart.
作者信息
Hu W M, Man R Y
机构信息
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
出版信息
Br J Pharmacol. 1991 Dec;104(4):773-5. doi: 10.1111/j.1476-5381.1991.tb12504.x.
Selectivity for blocking the coronary vasodilator and vasoconstrictor effects of platelet-activating factor (PAF) in the rat perfused heart was observed with different PAF antagonists. CV-6209 showed selectivity for blocking the vasodilator effect of PAF and a higher concentration (10 fold) was required to block the vasoconstrictor effect. The remaining PAF antagonists (FR-900452, WEB 2086 and BN-50739) showed selectivity for blocking the vasoconstrictor effect of PAF (10, 200 and 1000 fold respectively). A combination of low concentrations of CV-6209 (10 nM) with FR-900452 (5 microM) or WEB 2086 (0.5 microM) was effective in blocking both the vasodilator and vasoconstrictor effects of PAF. CV-6209 and WEB 2086 did not affect the vasodilator action of leukotriene B4 (LTB4) and the vasoconstrictor action of LTC4 and LTD4. Our results support the hypothesis that the functionally opposite effects of PAF in the rat perfused heart may be mediated by different PAF receptor subtypes.
使用不同的血小板活化因子（PAF）拮抗剂，观察到其对大鼠离体心脏中PAF的冠状动脉舒张和收缩作用具有选择性阻断作用。CV - 6209对PAF的舒张血管作用具有选择性阻断作用，而阻断其收缩血管作用则需要更高的浓度（高10倍）。其余的PAF拮抗剂（FR - 900452、WEB 2086和BN - 50739）对PAF的收缩血管作用具有选择性阻断作用（分别为高10、200和1000倍）。低浓度的CV - 6209（10 nM）与FR - 900452（5 microM）或WEB 2086（0.5 microM）联合使用可有效阻断PAF的舒张和收缩血管作用。CV - 6209和WEB 2086不影响白三烯B4（LTB4）的舒张血管作用以及白三烯C4（LTC4）和白三烯D4（LTD4）的收缩血管作用。我们的结果支持以下假说：PAF在大鼠离体心脏中功能相反的作用可能由不同的PAF受体亚型介导。
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