Affinity label for beta-adrenergic receptor in turkey erythrocytes.
The compound N-[2-hydroxy-3-(1-naphthoxy)-propyl]-N'-bromoacetylethylenediamine (NHNP-NBE) was found to label covalently the beta-adrenergic receptor in turkey erythrocytes. The compound inhibits irreversibly 1-epinephrine-dependent adenylate cyclase activity [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] in the whole turkey erythrocyte as well as in the erythrocyte membranes possessing the beta-receptor. The affinity label blocks, also irreversibly, the specific [3H] propranolol binding, whereas other bromoacetyl compounds tested have no effect on binding, even at high concentrations, which cause enzyme inactivation. 1-Epinephrine and propranolol offer protection against the affinity label in whole turkey erythrocytes as well as in membranes prepared from these cells. The potential usefulness of an irreversible beta-antagonist is discussed.
D000067956:Adenylyl Cyclase Inhibitors; D000345:Affinity Labels / Q000138:chemical synthesis / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D000242:Cyclic AMP / Q000096:biosynthesis; D004837:Epinephrine / Q000494:pharmacology; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism*; D007700:Kinetics; D011433:Propranolol / Q000378:metabolism; D011941:Receptors, Adrenergic; D014422:Turkeys
D000067956:Adenylyl Cyclase Inhibitors; D000345:Affinity Labels; D011941:Receptors, Adrenergic; D011433:Propranolol; D000242:Cyclic AMP; D004837:Epinephrine