Antioxidative Action of the β-Adrenoceptor Antagonist Bopindolol and Its Metabolite 18-502

[摘要] References(29)Cited-By(4)The antioxidative effects of β-adrenoceptor antagonists and related compounds were investigated. Among the β-adrenoceptor antagonists, the agents with a potent membrane-stabilizing activity such as bopindolol and propranolol strongly inhibited the hydrogen peroxide (H2O2)-induced lipid peroxidation of liver microsomes. Fifty percent inhibition concentration values for the lipid peroxidation of bopindolol, 18-502 (metabolite of bopindolol) and propranolol were calculated to be 1.8 μM, 10 μM and 2.3 μM, respectively. The same potency order of the agents for the inhibition of lipid peroxidation was observed in rat heart homogenates. Furthermore, cytochrome P-450-catalyzing lipid peroxidation in microsomes and H2O2-induced lipid peroxidation in coronary arteries or cardiac muscles of pigs were also inhibited by bopindolol, whereas propranolol was less effective. Bopindolol and 18-502, but not propranolol, scavenged a stable free radical 1, 1-diphenyl-2-picrylhydrazyl. Thus it was concluded that bopindolol that has membrane-stabilizing and radical scavenging activities is a more potent antioxidant than propranolol and may produce a beneficial effect for the treatment of ischemic cardiac diseases.

[学科分类] 药理学

[关键词] β-Adrenoceptor antagonist;Antioxidant;Bopindolol;Lipid peroxidation;Radical scavenger