Baker S P, Potter L T
Br J Pharmacol. 1980 Jan;68(1):8-10. doi: 10.1111/j.1476-5381.1980.tb10689.x.
The question of whether the chronic administration of propranolol modifies the numbers or properties of cardiac beta-adrenoceptors was examined because of many reports suggestive of cardiac hypersensitivity following the withdrawal of beta-antagonists. In three studies, rats were given (+/-)-propranolol, 30 mg/day, orally or intraperitoneally, for 1 to 7 weeks. The numbers and affinities of specific binding sites for radioactive dihydroalprenolol in whole hearts from 60 control and 75 test animals were found to be the same. Thus catecholamine deprivation does not exert an important regulatory effect on most beta-receptors in the heart, as it does in the brain.
由于许多报告提示β受体拮抗剂撤药后心脏会出现超敏反应,因此研究了长期给予普萘洛尔是否会改变心脏β肾上腺素能受体的数量或特性。在三项研究中,大鼠口服或腹腔注射(±)-普萘洛尔,剂量为30mg/天,持续1至7周。在60只对照动物和75只试验动物的全心脏中,放射性二氢阿普洛尔特异性结合位点的数量和亲和力相同。因此,儿茶酚胺缺乏对心脏中的大多数β受体不会像对大脑中的β受体那样产生重要的调节作用。