Bromoacetylalprenololmenthane binding to beta-receptors modulates the rate of hormone-induced internalization but not desensitization in S49 cells.
Bromoacetylalprenololmenthane was found to inhibit hormone-induced beta-adrenergic receptor internalization in a dose-dependent fashion in S49 lymphoma cells, besides its known ability to bind to beta-receptors irreversibly. This new found property of BAAM+ was taken advantage of in studying whether receptor internalization is a necessary step in the desensitization of adenylate cyclase. BAAM-treated cells showed functional desensitization even when receptor internalization had been blocked substantially by 50-65%. This finding suggests that receptor internalization is not directly involved in desensitization.
D000526:Alprenolol / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism; D007545:Isoproterenol / Q000494:pharmacology; D007700:Kinetics; D008223:Lymphoma / Q000378:metabolism; D011412:Propanolamines / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism*
D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C045331:bromoacetylalprenololmenthane; D000526:Alprenolol; D000242:Cyclic AMP; D007545:Isoproterenol; C033394:CGP 12177