Isoproterenol-initiated beta-adrenergic receptor diacytosis in cultured cells

The kinetics of the return of internalized beta-adrenergic receptors to the plasma membrane were measured in human astrocytoma cells. The movement of [125I]iodopindolol-labeled receptors back to the plasma membrane was measured directly and was shown to occur with a t1+2 of 3-4 min. Unlabeled receptors appeared to exhibit the same kinetics of externalization. The process was not inhibited by low concentrations (1-10 microM) of propranolol or even high concentrations of isoproterenol (0.1-1.0 mM). Higher concentrations of propranolol (0.1-1.0 mM) and other lipophilic amines inhibited externalization. The results are consistent with the proposal that catecholamine-induced beta-adrenergic receptor internalization and externalization (diacytosis) occur via the clathrin-coated pit/endosome pathway.