Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.
Journal Article (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
International Standard Serial Number (ISSN)
- 0022-2623
Digital Object Identifier (DOI)
- 10.1021/jm00232a018
Language
- eng
Conference Location
- United States