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Bisoprolol为一高选择性β_1-肾上腺素受体阻滞剂。一、药理放射性研究表明,(±)-bisoprolol 对β_1-受体有高度选择性,其亲合性较之对β_2-受体强100倍。生理学研究还发现它无内源性拟交感活性。本品拮抗离体人右心房β_1-受体的作用比拮抗β_2-受体强30倍。健康受试者体内试验表明,本品一日1次10 mg共9日不影响淋巴β_2-受体的密度。此外,健康受试者输注异丙基肾上腺素前30分
Bisoprolol is a highly selective β 1 -adrenoceptor blocker. First, pharmacological radioactivity studies have shown that (±) -bisoprolol is highly selective for β 1 -receptors and has 100-fold greater affinity than β 2 -receptors. Physiological studies also found that it has no endogenous sympathomimetic activity. This product antagonizes the right human atrial β 1-receptor role in antagonizing β 2-receptor 30 times stronger. In vivo tests of healthy subjects showed that the product once a day 10 mg on the 9th does not affect the density of lymphatic β 2 -receptors. In addition, healthy subjects were infused with isoproterenol for 30 minutes