7-SUBSTITUTED-2,3-DICHLORODIBENZO-PARA-DIOXINS AS COMPETITIVE LIGANDS FOR THE AH RECEPTOR - QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS (QSARS) AND A COMPARISON OF HUMAN RECEPTOR WITH AH RECEPTOR FROM RODENTS

被引：7

作者：

PROKIPCAK, RD

GOLAS, CL

MANCHESTER, DK

OKEY, AB

SAFE, S

FUJITA, T

机构：

[1] UNIV TORONTO, DEPT PHARMACOL, MED SCI BLDG, TORONTO M5S 1A8, ONTARIO, CANADA

[2] HOSP SICK CHILDREN, DIV CLIN PHARMACOL & TOXICOL, TORONTO M5G 1X8, ONTARIO, CANADA

[3] UNIV COLORADO, DEPT PEDIAT, DENVER, CO 80202 USA

[4] UNIV COLORADO, DEPT PHARMACOL, DENVER, CO 80202 USA

[5] UNIV COLORADO, DEPT PHARMACOL, DENVER, CO 80202 USA

[6] TEXAS A&M UNIV SYST, DEPT VET PHYSIOL & PHARMACOL, COLLEGE STN, TX 77843 USA

[7] KYOTO UNIV, DEPT AGR CHEM, KYOTO 606, JAPAN

来源：

CHEMOSPHERE | 1990年 / 20卷 / 7-9期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/0045-6535(90)90249-S

中图分类号：

X [环境科学、安全科学];

学科分类号：

08 ; 0830 ;

摘要：

The competitive binding affinities of thirteen 7-substituted-2,3,-dichlorodibenzo-p-dioxins to the human Ah placental cytosolic Ah receptor were determined versus [3H]-2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) as the radioligand. Multiple parameter linear regression analysis of the competitive binding EC50 values for these compounds gave the following equation: pEC50 (M)=6.246+1.632 π - 1.764σm° + 1.282 HB. were π is the substituent lipophilicity, σm° the meta-directing electronegativity and HB the hydrogen binding capacity. The equation obtained using human placental receptor was different than correlations previously derived for the binding of the same series of compounds to the rat, mouse, guinea pig or hamster cytosolic Ah receptor, providing further evidence for interspecies differences in the properties of the Ah receptor protein. © 1990.

引用

页码：1221 / 1228

页数：8

共 26 条

[1] COMPETITIVE-BINDING TO THE CYTOSOLIC 2,3,7,8-TETRACHLORODIBENZO-PARA-DIOXIN RECEPTOR - EFFECTS OF STRUCTURE ON THE AFFINITIES OF SUBSTITUTED HALOGENATED BIPHENYLS - A QSAR ANALYSIS [J].