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Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody.

Publication ,  Journal Article
Pitha, J; Zjawiony, J; Lefkowitz, RJ; Caron, MG
Published in: Proc Natl Acad Sci U S A
April 1980

The beta-adrenergic antagonist, alprenolol, was attached in an irreversible manner to macromolecular dextran via side arms that differed in length. The ability of these macromolecules to bind to the beta-adrenergic receptor of frog erythrocytes and to catecholamine-binding antibodies raised against partially purified receptors was studied. Compared to the parent drug the potency of binding of macromolecular alprenolol to the receptor decreased about 1/10, 1/600, and 1/8000 when the length of the arm separating alprenolol from the dextran moiety was 13, 8, and 4 atoms, respectively. In contrast, the binding potencies of the parent drug and of all its macromolecular derivatives for the antibody were within the same order of magnitude. Thus, conversion of a drug to a macromolecular form may not only sustain its binding activity but may also lead in a higher selectivity. The macromolecular derivatives described here may be suitable probes for investigation of the location and of the molecular properties of the binding sites for beta-adrenergic drugs.

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Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

April 1980

Volume

77

Issue

4

Start / End Page

2219 / 2223

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Molecular Weight
  • Kinetics
  • Dextrans
  • Binding Sites, Antibody
  • Binding Sites
  • Antibodies
  • Alprenolol
 

Citation

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Pitha, J., Zjawiony, J., Lefkowitz, R. J., & Caron, M. G. (1980). Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody. Proc Natl Acad Sci U S A, 77(4), 2219–2223. https://doi.org/10.1073/pnas.77.4.2219
Pitha, J., J. Zjawiony, R. J. Lefkowitz, and M. G. Caron. “Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody.Proc Natl Acad Sci U S A 77, no. 4 (April 1980): 2219–23. https://doi.org/10.1073/pnas.77.4.2219.
Pitha J, Zjawiony J, Lefkowitz RJ, Caron MG. Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody. Proc Natl Acad Sci U S A. 1980 Apr;77(4):2219–23.
Pitha, J., et al. “Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody.Proc Natl Acad Sci U S A, vol. 77, no. 4, Apr. 1980, pp. 2219–23. Pubmed, doi:10.1073/pnas.77.4.2219.
Pitha J, Zjawiony J, Lefkowitz RJ, Caron MG. Macromolecular beta-adrenergic antagonists discriminating between receptor and antibody. Proc Natl Acad Sci U S A. 1980 Apr;77(4):2219–2223.
Journal cover image

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

April 1980

Volume

77

Issue

4

Start / End Page

2219 / 2223

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Molecular Weight
  • Kinetics
  • Dextrans
  • Binding Sites, Antibody
  • Binding Sites
  • Antibodies
  • Alprenolol