Bromoacetylalprenololmenthane binding to beta-receptors modulates the rate of hormone-induced internalization but not desensitization in S49 cells

  • FEBS Lett. 1987 Apr 20;214(2):323-6. doi: 10.1016/0014-5793(87)80079-0.
R J Box M Staehelin
Abstract

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.

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