Trafficking of α1B-adrenergic receptor mediated by inverse agonist in living cells

• 作者: Chi-deHAN MingXU NingXU Shu-yiWang Xin-shengZHAO YaoSONG Ying-huaGUAN You-yiZHANG Zhang-yiLIANG
• 来源期刊: 中国药理通讯
• 学科: 医学
• 关键词: α1B-肾上腺素 受体作用 肝细胞 AR
• 年，卷（期）: 2005,（2）
• 页码范围: 24
• 页数: 1页
• 分类号: R975

摘要

AIM The project is aimed at understanding the action of inverse agonist at single molecule level and capturing the real time picture of molecular behavior of α1B-adrenergic receptor (AR) mediated by inverse agonist in living cells by single molecule detection (SMD). METHODS The location and distribution of α1B-AR was detected by laser confocal and whole cell ^3H-prazosin binding assay. Dynamic imaging of BODIPY-FL-labeled prazosin (Praz), specific antagonist of (1-AR, was observed in α1B-AR stably expressed human embryonic kidney 293 (HEK293) living cells. The detection of real-time dynamic behaviors of AR was achieved by using fluorescence-labeled AR and its ligand combined with SMD techniques. RESULTS α1B-AR was predominantly distributed on the cell surface and 8.2% of the total receptors were located in cytosol.