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用α1A-肾上腺素受体色谱研究哌嗪类化合物的生物亲和作用
王宏飞,杨晴来,左正龙,申旭霁,赵新锋,郑晓晖*
0
(西北大学中草药现代化工程研究中心,西安 710069)
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。
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 α1AAR(α1Aadrenocepter) chromatography for studying the biological affinity of piperazine compounds. MethodsAffinity 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. ResultsBiological 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. Conclusionα1AAR 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