文章基本信息

标题：A Fraction of the Ventricular Myocardium That Has the Specificity of the Cardiac Beta-Adrenergic Receptor
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作者：Robert J. Lefkowitz ; Edgar Haber
期刊名称：Proceedings of the National Academy of Sciences
印刷版ISSN：0027-8424
电子版ISSN：1091-6490
出版年度：1971
卷号：68
期号：8
页码：1773-1777
DOI：10.1073/pnas.68.8.1773
语种：English
出版社：The National Academy of Sciences of the United States of America
摘要：The 78,000 x g microsomal fraction of canine ventricular myocardium effected a 20-fold concentration of [3H]norepinephrine from a 10-9 M solution. The [3H]norepinephrine bound was displaced by physiologic concentrations of the beta-adrenergic catecholamines isoproterenol, epinephrine, and norepinephrine, in that order, which is the order of effectiveness of their actions on the force and rate of cardiac contraction. Alpha-adrenergic compounds did not displace [3H]norepinephrine until concentrations four orders of magnitude greater were reached. The beta-adrenergic blocker propranolol displaced at 10-6 M, whereas the alpha-adrenergic blocker phentolamine was inactive. Metabolites of the catecholamines did not compete for this binding site. It is concluded that, on the basis of specificity and affinity of binding, these microsomal particles are likely to contain the beta-adrenergic receptor.
关键词：norepinephrine binding ; displacement