IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科
学科主题临床医学
Thermodynamic study of the interaction between terbutaline and salbutamol with an immobilized beta(2)-adrenoceptor by high-performance liquid chromatography
Zhaoa, Xinfeng1,2; Zheng, Xiaohui2; Wei, Yinmao2; Bian, Liujiao2; Wang, Shixiang2; Zheng, Jianbin2; Zhang, Youyi3,4; Li, Zijian3,4; Zang, Weijin1
关键词beta(2)-Adrenoceptor Terbutaline Salbutamol Zonal elution Thermodynamics
刊名JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
2009-04-01
DOI10.1016/j.jchromb.2009.02.031
877期:10页:911-918
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Chemistry, Analytical
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]PROTEIN-COUPLED RECEPTOR ; HUMAN SERUM-ALBUMIN ; STATIONARY-PHASE ; NONCOMPETITIVE INHIBITORS ; AFFINITY-CHROMATOGRAPHY ; BETA-AGONISTS ; BINDING ; DISPLACEMENT ; ANTAGONISTS ; CONSTANTS
英文摘要

Investigation of the interaction between drugs and receptors is very important in revealing the biologic basis and mechanism of the drug, and designing new bioactive compounds. The beta(2)-adrenoceptor (beta(2)-AR) was purified from rabbit lung tissues and immobilized on the surface of macro-pore silica gel through covalent bonds to prepare the stationary phase. Binding isotherms of terbutaline and salbutamol were determined by frontal analysis and the perturbation method, respectively. On the basis of the model of binding isotherm assumed, zonal elution was used to investigate the binding interaction of the receptor with terbutaline and salbutamol. The two drugs had one type of common binding site on immobilized beta(2)-AR. Salbutamol had at least one other major binding region. The association constant for terbutaline was (9.76 +/- 0.67) x 10(4)/M, and the concentration of the binding sites was (9.37 +/- 1.32) x 10(-6) M. Under identical conditions, association constants for salbutamol at the two types of binding site were (1.11 +/- 0.08) x 10(4)/M and (1.34 +/- 0.13) x 10(3)/M, and the concentration of the binding sites was (5.46 +/- 0.35) x 10(-6) M. Entropy increase was the main driving force for terbutaline and salbutamol to bind with beta(2)-AR. The associating reaction of terbutaline and beta(2)-AR was an exothermal process primarily from electrostatic interactions; hydrophobic force was the major factor contributing to the process for salbutamol. (C) 2009 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000265130100009
项目编号20875074 ; 20875075 ; 20575052 ; 30770785 ; 2007CB512005 ; 705045 ; 2007DF02
资助机构National Natural Science Foundation of China ; National Basic Research Program of China ; Chinese Ministry of Education ; Chinese Academy of Sciences
引用统计
被引频次:31[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/63035
专题北京大学第三临床医学院_心血管内科
作者单位1.Minist Educ, Key Lab Mol Cardiovasc Sci, Beijing 100083, Peoples R China
2.Xi An Jiao Tong Univ, Sch Med, Key Lab Environm & Genes Related Dis, Minist Educ,Dept Pharmacol, Xian 710061, Shaanxi, Peoples R China
3.NW Univ Xian, Shaanxi Prov Key Lab Electroanalyt Chem, Xian 710069, Peoples R China
4.Peking Univ, Hosp 3, Inst Vasc Med, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Zhaoa, Xinfeng,Zheng, Xiaohui,Wei, Yinmao,et al. Thermodynamic study of the interaction between terbutaline and salbutamol with an immobilized beta(2)-adrenoceptor by high-performance liquid chromatography[J]. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,2009,877(10):911-918.
APA Zhaoa, Xinfeng.,Zheng, Xiaohui.,Wei, Yinmao.,Bian, Liujiao.,Wang, Shixiang.,...&Zang, Weijin.(2009).Thermodynamic study of the interaction between terbutaline and salbutamol with an immobilized beta(2)-adrenoceptor by high-performance liquid chromatography.JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,877(10),911-918.
MLA Zhaoa, Xinfeng,et al."Thermodynamic study of the interaction between terbutaline and salbutamol with an immobilized beta(2)-adrenoceptor by high-performance liquid chromatography".JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES 877.10(2009):911-918.
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