Box R J, Staehelin M
FEBS Lett. 1987 Apr 20;214(2):323-6. doi: 10.1016/0014-5793(87)80079-0.
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.
除了已知的不可逆结合β受体的能力外,还发现溴乙酰阿普洛尔薄荷烷能以剂量依赖的方式抑制S49淋巴瘤细胞中激素诱导的β肾上腺素能受体内化。利用BAAM +的这一新发现特性,研究受体内化是否是腺苷酸环化酶脱敏的必要步骤。即使受体内化已被50%-65%显著阻断,经BAAM处理的细胞仍表现出功能性脱敏。这一发现表明受体内化与脱敏没有直接关系。