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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 study the bioaffinity of piperazine and α1A-AR by α1A-adrenergic receptor (α1A-AR). Methods α1A-AR was purified from rabbit heart tissue by affinity chromatography. The macroporous silica gel was used as a carrier and the α1A-AR was covalently immobilized on the macropores The surface of silica gel was characterized by using terazosin hydrochloride, norepinephrine, tamsulosin, m-hydroxylamine and urapidil for the retention ofα1A-AR column. Six kinds of piperazine compounds were chemically synthesized and studied by the chromatographic model Its interaction with α1A-AR. Results The biosynthesis of the synthesized piperazines with α1A-AR showed that the affinities were as follows: compound 3> compound 4> compound 1> compound 2> compound 5> compound 6. Conclusion α1A-AR chromatography is a specific and reliable bioaffinity chromatography method that can be used for the preliminary study of drug activity.