Fukunaga H, Saito K, Tanaka H
First Department of Internal Medicine, Faculty of Medicine, Kagoshima University, Japan.
Jpn Heart J. 1990 Sep;31(5):693-701. doi: 10.1536/ihj.31.693.
We have studied the effects of propranolol on the number and function of beta-adrenoceptors of cultured heart cells from mice. After 24 hrs in culture, heart cells were incubated for 48 hrs with either standard medium or medium containing propranolol. After a washing period of 30 min, beta-adrenoceptors were measured with a receptor binding assay. The dissociation constant (Kd) did not differ between control and cultured heart cells pretreated with propranolol. By contrast, the maximum number of binding sites (Bmax) was 2.5 times higher in propranolol-pretreated than control cultured heart cells. The increase in the rate of beating and the elevation of cyclic AMP content induced by 10(-5) M isoproterenol were significantly higher for cultured cells pretreated with propranolol than for control cells. These results indicate a correlation between an increased number of beta-adrenoceptors and increased physiological responses of cultured heart cells after propranolol withdrawal.
我们研究了普萘洛尔对培养的小鼠心脏细胞β-肾上腺素能受体数量和功能的影响。培养24小时后,将心脏细胞与标准培养基或含普萘洛尔的培养基一起孵育48小时。经过30分钟的洗涤期后,用受体结合试验测定β-肾上腺素能受体。对照和用普萘洛尔预处理的培养心脏细胞之间的解离常数(Kd)没有差异。相比之下,用普萘洛尔预处理的培养心脏细胞的最大结合位点数(Bmax)比对照高2.5倍。对于用普萘洛尔预处理的培养细胞,10^(-5) M异丙肾上腺素诱导的搏动速率增加和环磷酸腺苷含量升高显著高于对照细胞。这些结果表明,在停用普萘洛尔后,培养的心脏细胞中β-肾上腺素能受体数量增加与生理反应增强之间存在相关性。