Bufetololのラット心臓および肝臓Adenyl Cyclase活性に対する作用

概要

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The effect of bufetolol, a β-adrenergic blocking agent, on the activities of the adenyl cyclase of rat heart (β_1) and liver (β_2) was examined. Bufetolol did not activate adenyl cyclase of the heart at concentrations from 10^<-5> to 10^<-10>M, but showed a slight inhibition at high concentrations. Bufetolol inhibited the activation of heart adenyl cyclase by 10^<-5>M epinephrine or isoproterenol at above 10^<-9> or 10^<-6>M, respectively, but did not inhibit the activation by 3μg/ml of glucagon or 10^<-3>M of NaF. The inhibition of Bufetolol against isoproterenol was shown to be competetive from Lineweaver-Burk analysis. Bufetolol did not affect the basal activity of the liver adenyl cyclase. With the activation by 10^<-5>M epinephrine, bufetolol inhibited it at 10^<-6>M or higher concentrations. The activities of phosphodiesterase and Mg^<2+>, Na^+, K^+-adenosine triphosphatase of rat heart or protein kinase of rabbit skeletal muscle were not affected by bufetolol. These results suggest that the β-adrenergic blocking activity of Bufetolol is shown by the inhibition of the activation of adenyl cyclase in competition with catecholamines at β-receptor sites.
公益社団法人日本薬学会の論文
1976-05-25