| Title | Investigation on the Binding of Terazosin Hydrochloride and Naftopidil to an Immobilized alpha (1)-Adrenoceptor by Zonal Elution |
| Authors | Gao, Xiaokang Li, Qian Zhao, Xinfeng Huang, Jingjing Bian, Liujiao Zheng, Jianbin Li, Zijian Zhang, Youyi Zheng, Xiaohui |
| Affiliation | NW Univ Xian, Key Lab Resource Biol & Biotechnol Western China, Minist Educ, Xian 710069, Peoples R China. NW Univ Xian, Inst Analyt Sci, Xian 710069, Shaanxi, Peoples R China. Peking Univ, Inst Vasc Med, Hosp 3, Beijing 100083, Peoples R China. Minist Educ, Key Lab Mol Cardiovasc Sci, Beijing 100083, Peoples R China. |
| Keywords | alpha(1)-Adrenoceptor High-performance affinity chromatography Naftopidil Terazosin hydrochloride PERFORMANCE AFFINITY-CHROMATOGRAPHY BENIGN PROSTATIC HYPERPLASIA HUMAN SERUM-ALBUMIN CARBAMAZEPINE BINDING INTERNATIONAL UNION NOMENCLATURE PHARMACOLOGY |
| Issue Date | 2014 |
| Citation | CHROMATOGRAPHIA.2014/9/1,77(1235-1239). |
| Abstract | The interaction between drugs and receptors is particularly important in revealing the drug acting mechanism and developing new leads. In this work, alpha (1)-Adrenoceptor (alpha (1)-AR) from HEK293 cell line is purified and immobilized on the surface of macro-pore silica gel to prepare an high-performance affinity chromatography stationary phase for the pursuit of drug-receptor interactions by competition zonal elution. Naftopidil is found to have only one type of binding site to alpha (1)-AR with an association constant of 1.45 x 10(6) M-1 and a concentration of binding sites of 1.56 x 10(-6) M, while terazosin hydrochloride proves to present two kinds of binding site on the receptor at which the association constants are determined to be 1.61 x 10(5) M-1 and 2.06 x 10(3) M-1, and the corresponding concentrations of the binding sites are 1.56 x 10(-6) M and 1.11 x 10(-3) M, respectively. It is concluded that the stationary phase containing attached alpha (1)-AR can be used to realize the binding of a drug to the receptor. |
| URI | http://hdl.handle.net/20.500.11897/209005 |
| ISSN | 0009-5893 |
| DOI | 10.1007/s10337-014-2716-7 |
| Indexed | SCI(E) CPCI-S(ISTP) |
| Appears in Collections: | 第三医院 |
