| 摘要: |
| 目的用α1A肾上腺素受体(α1AAR)色谱法研究哌嗪类化合物与α1AAR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α1AAR, 以大孔硅胶为载体, 采用温和的化学偶联方法, 将α1AAR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α1AAR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α1AAR之间的相互作用关系。结果所合成哌嗪类化合物与α1AAR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α1AAR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。 |
| 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 |
| DOI：10.3724/SP.J.1008.2011.058 |
| 投稿时间：2010-07-17修订日期：2010-12-12 |
| 基金项目:国家自然科学基金(20875074/b0501). |
|
| α1A-Adrenocepter chromatography in studying biological affinity of piperazine compounds |
| WANG Hong-fei,YANG Qing-lai,ZUO Zheng-long,SHEN Xu-ji,ZHAO Xin-feng,ZHENG Xiao-hui* |
| (Research Center of Chinese Herbal Medicine Modernization, Northwest University, Xi’an 710069, Shaanxi, China) |
| Abstract: |
| ObjectiveTo use α1AAR(α1Aadrenocepter) chromatography for studying the biological affinity of piperazine compounds. MethodsAffinity chromatography was used to purify α1AAR obtained from rabbit heart. α1AAR was immobilized on macroporous silica through the covalent bond by mild chemical coupling methods. The retention characteristics of α1AAR column were investigated with terazosin, norepinephrine, tamsulosin, metaraminol, and urapidil. Six piperazine compounds were synthesized, and the interactions between the compounds and α1AAR were investigated by the chromatographic model. ResultsBiological affinity was found between the synthesized piperazine compounds and α1AAR,with the order of affinity intensities being compound 3＞compound 4＞compound 1＞compound 2＞compound 5＞compound 6. Conclusionα1AAR chromatography is a specific and reliable biological affinity chromatography and can be used for preliminary study of drug activity. |
| Key words: adrenocepter α1 piperazines affinity chromatography biological affinity |
