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.