Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.

Journal Article

Spin-labeled analogues of dichloroisoproterenol and propranolol were synthesized. It was found that the KD's of both probes for the beta-adrenergic receptors of frog erythrocytes were about 30-fold higher than the KD's previously reported for the parent antagonists. Thus the introduction of a bulky nitroxide moiety in place of the isopropyl group on the amino nitrogen is associated with a decrease in affinity for the beta-adrenergic receptors. Nonetheless, the affinity of the spin-labeled propranolol would appear to be within a range compatible with EPR measurements.

Full Text

Duke Authors

Cited Authors

  • Rauckman, EJ; Rosen, GM; Lefkowitz, RJ

Published Date

  • October 1, 1976

Published In

Volume / Issue

  • 19 / 10

Start / End Page

  • 1254 - 1256

PubMed ID

  • 11346

Pubmed Central ID

  • 11346

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm00232a018

Language

  • eng

Conference Location

  • United States