Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol.
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.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000526:Alprenolol / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D004912:Erythrocytes / Q000378:metabolism / Q000648:ultrastructure; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011433:Propranolol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011894:Rana pipiens; D011943:Receptors, Adrenergic, beta; D013113:Spin Labels / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D011943:Receptors, Adrenergic, beta; D013113:Spin Labels; D000526:Alprenolol; D011433:Propranolol; D000262:Adenylyl Cyclases; D007545:Isoproterenol