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Adenylate cyclase coupled beta adrenergic receptors effect of membrane lipid perturbing agents on receptor binding and enzyme stimulation by catecholamines



Adenylate cyclase coupled beta adrenergic receptors effect of membrane lipid perturbing agents on receptor binding and enzyme stimulation by catecholamines



Molecular Pharmacology 12(4): 559-567



Binding of (-)-[3H]dihydroalprenolol, a potent competitive .beta.-adrenergic antagonist, to sites in frog erythrocyte membranes was previously demonstrated to possess the essential properties expected of binding to adenylate cyclase-coupled .beta.-adrenergic receptors. The effects of a variety of membrane lipid-perturbing agents on both .beta.-adrenergic receptor binding and catecholamine-responsive adenylate cyclase in frog erythrocyte membranes were tested. Digestion of membranes with phospholipases A, C and D causes a dose-dependent decline in receptor binding capacity without altering receptor affinity. Amphotericin B, a nondegradative membrane lipid perturbant, causes a dose-dependent decrease in (-)-[3H]dihydroalprenolol binding. Decrements in catecholamine-stimulated adenylate cyclase activity caused by these agents are always greater than decreases in basal and Fl-sensitive enzyme activities. Decreases in (-)-[3H]dihydroalprenolol binding parallel the disproportionate reduction in catecholamine responsiveness of adenylate cyclase. The polyene antibiotic Filipin appears to uncouple receptor binding and enzyme activation, since a marked reduction in isoproterenol-stimulated adenylate cyclase is not accompanied by a decrease in specific (-)-[3H]dihydroalprenolol binding.

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Accession: 004677792

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PMID: 958206


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