Exercise‐Induced Increase in Plasma Arachidonic Acid and Thromboxane B2 in Healthy Men: Effect of β-Adrenergic Blockade

Exercise‐Induced Increase in Plasma Arachidonic Acid and Thromboxane B2 in Healthy Men: Effect of β-Adrenergic Blockade
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运动引起的健康男性血浆花生四烯酸和血栓素 B2 增加:β-肾上腺素能阻断的作用

DOI:
10.1097/00005344-198405000-00012
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发表时间:
1984
影响因子:
3
通讯作者:
H. Vapaatalo
H. Vapaatalo
中科院分区:
医学4区
文献类型:
--
作者:
K. Laustiola;Erkki Seppala;T. Nikkari;H. Vapaatalo

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我们研究了非选择性拮抗剂普萘洛尔、心脏选择性拮抗剂阿替洛尔和具有部分激动活性的心脏选择性拮抗剂普奈洛尔的 β-阻滞剂对六名正常受试者血浆中游离花生四烯酸 (AA)、血栓素 B2 (TxB2)、前列腺素 (PG) E2 和 6-酮-PGF1α 水平以及凝血过程中血小板产生的 TxB2 的影响。在次最大动态运动期间。在运动试验前,以等量递增剂量静脉注射药物。运动导致血浆中 AA、TxB2 和 6-keto-PGF1α 明显增加。在运动的前 60 分钟内,所有三种 β 受体阻滞剂均降低了 AA 和 TxB2 的血浆水平。普萘洛尔(0.19 mg/kg)比阿替洛尔(0.19 mg/kg)或普奈洛尔(0.64 mg/kg)稍有效;然而,在力竭时,普萘洛尔明显比其他两种阻滞剂更有效。运动期间血浆 6-酮-PGF1α 和 PGE2 水平受 β-阻断的影响较小,并且对血小板形成 TxB2 没有显着影响。运动期间,普萘洛尔治疗后血浆6-酮-PGF1α/TxB2比值明显高于其他两种阻滞剂治疗后。这些结果表明,非选择性阻滞剂抑制 β1 和 β2 肾上腺素能受体的能力可能是有利的,因为它比心脏选择性阻滞剂更有效地抑制血栓素形成,特别是当交感神经张力显着增加时。
We examined the effects of β-blockade with the nonselective antagonist propranolol, the cardioselective antagonist atenolol, and the cardioselective antagonist with partial agonist activity, practolol, on the levels of free arachidonic acid (AA), thromboxane B2 (TxB2), prostaglandin (PG) E2, and 6-keto-PGF1α in plasma, and TxB2 production by platelets during clotting in six normal subjects during sub-maximal dynamic exercise. The drugs were given intravenously in equipotent increasing doses before the exercise test. Exercise induced a clear increase in AA, TxB2, and 6-keto-PGF1α in plasma. During the first 60 min of exercise all three β-blockers decreased the plasma levels of AA and TxB2. Propranolol (0.19 mg/kg) was slightly more effective than atenolol (0.19 mg/kg) or practolol (0.64 mg/kg); however, at exhaustion, propranolol was markedly more effective than the other two blockers. Plasma 6-keto-PGF1α and PGE2 levels were less affected by β-blockade during exercise, and no significant effect was seen on TxB2 formation by platelets. The plasma 6-keto-PGF1α/TxB2 ratio was markedly higher after propranolol treatment than after treatment with the other two blockers during the exercise period. These results suggest that the capability of a nonselective blocker to inhibit both β1- and β2-adrenergic receptors may be of advantage because of the more effective inhibition of thromboxane formation than with a cardioselective blocker, especially when the sympathetic tone is markedly increased.