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Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding.

Publication ,  Journal Article
Stiles, GL; Taylor, S; Lefkowitz, RJ
Published in: Life Sci
August 1, 1983

Human myocardial beta-adrenergic receptors were directly identified and characterized using the high affinity antagonist radioligand [125I]iodocyanopindolol. Beta 1 and beta 2 adrenergic receptors were found to coexist in both the left ventricle and right atrium. The relative proportions of the two receptor subtypes were determined by the use of competition radioligand binding and computer modelling techniques employing the subtype selective agents atenolol (beta 1 selective) and zinterol (beta 2 selective). The left ventricle contains 86 +/- 1% beta 1 and 14 +/- 1% beta 2 adrenergic receptors while the right atrium contains 74 +/- 6% beta 1 and 26 +/- 6% beta 2 adrenergic receptors. The direct demonstration of beta 2 adrenergic receptors in the human heart, with a higher proportion in the right atrium agrees with pharmacologic data and supports the notion that chronotropic effects of adrenergic agonists in man may be mediated by both beta 1 and beta 2 adrenergic receptors.

Duke Scholars

Published In

Life Sci

DOI

ISSN

0024-3205

Publication Date

August 1, 1983

Volume

33

Issue

5

Start / End Page

467 / 473

Location

Netherlands

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Radioligand Assay
  • Pindolol
  • Pharmacology & Pharmacy
  • Myocardium
  • Kinetics
  • Iodocyanopindolol
  • Humans
  • Binding, Competitive
 

Citation

APA
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ICMJE
MLA
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Stiles, G. L., Taylor, S., & Lefkowitz, R. J. (1983). Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding. Life Sci, 33(5), 467–473. https://doi.org/10.1016/0024-3205(83)90796-8
Stiles, G. L., S. Taylor, and R. J. Lefkowitz. “Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding.Life Sci 33, no. 5 (August 1, 1983): 467–73. https://doi.org/10.1016/0024-3205(83)90796-8.
Stiles GL, Taylor S, Lefkowitz RJ. Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding. Life Sci. 1983 Aug 1;33(5):467–73.
Stiles, G. L., et al. “Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding.Life Sci, vol. 33, no. 5, Aug. 1983, pp. 467–73. Pubmed, doi:10.1016/0024-3205(83)90796-8.
Stiles GL, Taylor S, Lefkowitz RJ. Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding. Life Sci. 1983 Aug 1;33(5):467–473.
Journal cover image

Published In

Life Sci

DOI

ISSN

0024-3205

Publication Date

August 1, 1983

Volume

33

Issue

5

Start / End Page

467 / 473

Location

Netherlands

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Radioligand Assay
  • Pindolol
  • Pharmacology & Pharmacy
  • Myocardium
  • Kinetics
  • Iodocyanopindolol
  • Humans
  • Binding, Competitive