A fraction of the ventricular myocardium that has the specificity of the cardiac beta-adrenergic receptor.

Published

Journal Article

The 78,000 x g microsomal fraction of canine ventricular myocardium effected a 20-fold concentration of [(3)H]norepinephrine from a 10(-9) M solution. The [(3)H]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 [(3)H]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.

Full Text

Duke Authors

Cited Authors

  • Lefkowitz, RJ; Haber, E

Published Date

  • August 1, 1971

Published In

Volume / Issue

  • 68 / 8

Start / End Page

  • 1773 - 1777

PubMed ID

  • 4399664

Pubmed Central ID

  • 4399664

International Standard Serial Number (ISSN)

  • 0027-8424

Digital Object Identifier (DOI)

  • 10.1073/pnas.68.8.1773

Language

  • eng

Conference Location

  • United States