用α_(1A)-肾上腺素受体色谱研究哌嗪类化合物的生物亲和作用  

α_(1A)-Adrenocepter chromatography in studying biological affinity of piperazine compounds

作　　者：王宏飞[1] 杨晴来[1] 左正龙[1] 申旭霁[1] 赵新锋[1] 郑晓晖[1] 

机构地区：[1]西北大学中草药现代化工程研究中心,西安710069

出　　处：《第二军医大学学报》2011年第1期58-61,共4页Academic Journal of Second Military Medical University

基　　金：国家自然科学基金(20875074/b0501)~~

摘　　要：目的用α1A-肾上腺素受体(α1A-AR)色谱法研究哌嗪类化合物与α1A-AR的生物亲和作用。方法采用亲和层析色谱法从家兔心脏组织中纯化得到α1A-AR,以大孔硅胶为载体,采用温和的化学偶联方法,将α1A-AR通过共价键均匀地固载在大孔硅胶表面,用盐酸特拉唑嗪、去甲肾上腺素、坦索罗辛、间羟胺和乌拉地尔表征α1A-AR色谱柱的保留特性;化学合成6种哌嗪类化合物,并用该色谱模型研究其与α1A-AR之间的相互作用关系。结果所合成哌嗪类化合物与α1A-AR之间有生物亲和作用,其亲和力大小为:化合物3>化合物4>化合物1>化合物2>化合物5>化合物6。结论α1A-AR色谱法是一种特异、可靠的生物亲和色谱方法,可用于药物活性的初步研究。Objective To use α1A-AR（α1A-adrenocepter） chromatography for studying the biological affinity of piperazine compounds.Methods Affinity chromatography was used to purify α1A-AR obtained from rabbit heart.α1A-AR was immobilized on macroporous silica through the covalent bond by mild chemical coupling methods.The retention characteristics of α1A-AR column were investigated with terazosin,norepinephrine,tamsulosin,metaraminol,and urapidil.Six piperazine compounds were synthesized,and the interactions between the compounds and α1A-AR were investigated by the chromatographic model.Results Biological affinity was found between the synthesized piperazine compounds and α1A-AR,with the order of affinity intensities being compound 3 compound 4 compound 1 compound 2 compound 5 compound 6.Conclusion α1A-AR chromatography is a specific and reliable biological affinity chromatography and can be used for preliminary study of drug activity.

关 键 词：肾上腺素能α1受体 哌嗪类 亲和色谱法 生物亲和作用 

分 类 号：R917.74[医药卫生—药物分析学]