Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.
Publication
, Journal Article
Rauckman, EJ; Rosen, GM; Lefkowitz, RJ
Published in: J Med Chem
October 1976
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.
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Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
October 1976
Volume
19
Issue
10
Start / End Page
1254 / 1256
Location
United States
Related Subject Headings
- Structure-Activity Relationship
- Spin Labels
- Receptors, Adrenergic, beta
- Rana pipiens
- Propranolol
- Medicinal & Biomolecular Chemistry
- Isoproterenol
- In Vitro Techniques
- Erythrocytes
- Binding, Competitive
Citation
APA
Chicago
ICMJE
MLA
NLM
Rauckman, E. J., Rosen, G. M., & Lefkowitz, R. J. (1976). Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol. J Med Chem, 19(10), 1254–1256. https://doi.org/10.1021/jm00232a018
Rauckman, E. J., G. M. Rosen, and R. J. Lefkowitz. “Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.” J Med Chem 19, no. 10 (October 1976): 1254–56. https://doi.org/10.1021/jm00232a018.
Rauckman EJ, Rosen GM, Lefkowitz RJ. Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol. J Med Chem. 1976 Oct;19(10):1254–6.
Rauckman, E. J., et al. “Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.” J Med Chem, vol. 19, no. 10, Oct. 1976, pp. 1254–56. Pubmed, doi:10.1021/jm00232a018.
Rauckman EJ, Rosen GM, Lefkowitz RJ. Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol. J Med Chem. 1976 Oct;19(10):1254–1256.
Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
October 1976
Volume
19
Issue
10
Start / End Page
1254 / 1256
Location
United States
Related Subject Headings
- Structure-Activity Relationship
- Spin Labels
- Receptors, Adrenergic, beta
- Rana pipiens
- Propranolol
- Medicinal & Biomolecular Chemistry
- Isoproterenol
- In Vitro Techniques
- Erythrocytes
- Binding, Competitive