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

[摘要]

Bromoacetylalprenololmenthane was found to inhibit hormone-induced β-adrenergic receptor internalization in a dose-dependent fashion in S49 lymphoma cells, besides its known ability to bind to β-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.

[学科分类] 生物化学/生物物理

[关键词] β-Adrenergic receptor;Desensitization;Receptor internalization;Internalization blockade;(S49 wild type cell);BAAM;bromoacetylalprenololmenthane;CGP-12177;4-(3-tert-butylamino-2-hydroxypropoxy)benzimidazole-2-one hydrochloride;DMEM;Dulbecco's modified Eagle's medium;IPR;(−)-iso-proterenol