中国药理学与毒理学杂志2003，Vol.17Issue(1)：70-73,4.
用细胞膜色谱法研究药物和毒蕈碱受体的亲和作用
Evaluation of drug-muscarinic receptor affinities by using cell membrane chromatography
侯进 1袁秉祥 2贺浪冲 3杨广德 3弥曼1
作者信息
- 1. 陕西医学高等专科学校药理学教研室, 陕西,西安,710068
- 2. 西安交通大学 医学院药理学教研室,陕西,西安,710061
- 3. 西安交通大学药学院, 陕西,西安,710061
- 折叠
摘要
Abstract
AIM To evaluate if cell membrane chromatography(CMC) can be used to reflect the selectivity and specificity of drug-muscarinic acetylcholine receptor (mAChR) interaction. METHODS The cell membrane stationary phase (CMSP) was prepared by immobilizing rat atrium cell membrane on the surface of a silica carrier and used for the rapid on-line chromatographic evaluation of ligand binding affinities to mAChR. RESULTS The capacity factor profiles in rat atrium CMSP were: (-)QNB(11.5)>pirenzepine(4.8)>atropine(4.2)>4-DAMP(3.5)>AF-DX116(2.4)>pilocarpine(1.14)>acetylcholine(1.02). Those results compared with the affinity rank orders obtained from radioligand binding assays using the same atrium tissue indicated there was a positive correlation (r=0.9, P<0.05) between the both data sets. However, there were some unusual capactity factors. CONCLUSION CMC method can be used to preliminarily evaluate drug-receptor affinities for drug candidates but the accuracy should be validated by traditional radioligand binding assay.关键词
色谱法,细胞膜/受体,毒蕈碱/放射免疫测定Key words
chromatography, cell membrane/receptors, muscarinic/radioimmunoassay分类
医药卫生引用本文复制引用
侯进,袁秉祥,贺浪冲,杨广德,弥曼..用细胞膜色谱法研究药物和毒蕈碱受体的亲和作用[J].中国药理学与毒理学杂志,2003,17(1):70-73,4.
