α1A-adrenocepter chromatography in studying biological affinity of piperazine compounds / 第二军医大学学报

ABSTRACT

Objective: To use α1A-AR (α1A- adrenoceptor) 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.