TY - JOUR
T1 - 7-Substituted-2,3-dichlorodibenzo-p-dioxins as competitive ligands for the Ah receptor
T2 - Quantitative structure-activity relationships (QSARs) and a comparison of human receptor with Ah receptor from rodents
AU - Prokipcak, Rebecca D.
AU - Golas, Cheryl L.
AU - Manchester, David K.
AU - Okey, Allan B.
AU - Safe, Steven
AU - Fujita, Toshio
N1 - Funding Information:
The financial assistance of the National Cancer Institute of Canada to A.B.O. and the National Institutes of Health (ES03554) to S.S. is gratefully acknowledged. S. Safe is a Burroughs Wellcome Toxicology Scholar (1989-1994).
PY - 1990
Y1 - 1990
N2 - 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.
AB - 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.
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U2 - 10.1016/0045-6535(90)90249-S
DO - 10.1016/0045-6535(90)90249-S
M3 - Article
AN - SCOPUS:0025179917
SN - 0045-6535
VL - 20
SP - 1221
EP - 1228
JO - Chemosphere
JF - Chemosphere
IS - 7-9
ER -