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卡维地洛是一种新型β-肾上腺素能受体拮抗剂和血管舒张性抗高血压药物,可抑制人中性粒细胞释放超氧化物。

Carvedilol, a new beta-adrenoceptor antagonist and vasodilator antihypertensive drug, inhibits superoxide release from human neutrophils.

作者信息

Yue T L, McKenna P J, Ruffolo R R, Feuerstein G

机构信息

Department of Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939.

出版信息

Eur J Pharmacol. 1992 Apr 22;214(2-3):277-80. doi: 10.1016/0014-2999(92)90130-v.

Abstract

Carvedilol produced a dose-dependent inhibition of superoxide (O2-) release from human neutrophils (PMNs) (IC50 = 28 microM) and scavenged O2- generated during dihydroxyfumaric acid (DHF) autooxidation (IC50 = 41 microM). Other beta-blockers, such as celiprolol, labetalol and atenolol, or the antioxidant, 'lazaroid', U74500A had no effect on O2- either released from PMNs or generated during DHF autooxidation. Propranolol, at 0.3 mM, inhibited O2- release from PMNs (73%) but failed to scavenge O2- generated from DHF. The novel free radical-scavenging effect of carvedilol may contribute to the cardioprotective activity of the compound.

摘要

卡维地洛对人中性粒细胞(PMN)释放超氧阴离子(O2-)产生剂量依赖性抑制作用(IC50 = 28微摩尔),并清除二羟基富马酸(DHF)自氧化过程中产生的O2-(IC50 = 41微摩尔)。其他β受体阻滞剂,如塞利洛尔、拉贝洛尔和阿替洛尔,或抗氧化剂“拉扎罗类药物”U74500A对PMN释放的O2-或DHF自氧化过程中产生的O2-均无影响。0.3毫摩尔的普萘洛尔抑制PMN释放O2-(73%),但未能清除DHF产生的O2-。卡维地洛新的自由基清除作用可能有助于该化合物的心脏保护活性。

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