Yue T L, Lysko P G, Barone F C, Gu J L, Ruffolo R R, Feuerstein G Z
Department of Cardiovascular Pharmacology SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406-0939.
Ann N Y Acad Sci. 1994 Nov 17;738:230-42. doi: 10.1111/j.1749-6632.1994.tb21808.x.
The antioxidant activities of carvedilol have been demonstrated in a wide variety of test systems, including (i) physicochemical (EPR studies), (ii) biochemical (measurement of lipid peroxidation and endogenous antioxidant depletion), (iii) cellular, and (iv) in vivo. The antioxidant activity of carvedilol clearly emanates from the carbazole moiety which is unique to carvedilol. The antioxidant activity resides equally in both of the enantiomers of carvedilol, as well as in some of its metabolites which are devoid of either the alpha 1-adrenoceptor blocking activity or beta-adrenoceptor blocking activity. This novel antioxidant property of carvedilol may account, at least in part, for its cerebroprotection. The data discussed in this article suggest that carvedilol may not only provide effective and safe antihypertensive therapy and therefore reduce a major risk factor for stroke, but will also be better able to provide additional benefits to patients by protecting against oxygen free radicals generated during cerebral ischemia and stroke.
卡维地洛的抗氧化活性已在多种测试系统中得到证实，包括：（i）物理化学（电子顺磁共振研究），（ii）生物化学（脂质过氧化和内源性抗氧化剂消耗的测量），（iii）细胞水平，以及（iv）体内研究。卡维地洛的抗氧化活性显然源自其独特的咔唑部分。卡维地洛的抗氧化活性在其两种对映体以及一些代谢产物中均有体现，这些代谢产物不具有α1肾上腺素能受体阻断活性或β肾上腺素能受体阻断活性。卡维地洛这种新的抗氧化特性可能至少部分地解释了其脑保护作用。本文所讨论的数据表明，卡维地洛不仅可以提供有效且安全的抗高血压治疗，从而降低中风的主要风险因素，而且通过抵御脑缺血和中风期间产生的氧自由基，还能够更好地为患者带来额外益处。
