Table 2.
Aryl hydrocarbon receptor (AHR) ligands
Ligand | EC50 (mol/kg) | Metabolized? | References |
---|---|---|---|
HAH (TCDD) | 10−12 | No | 116,117 |
PAH (BaP) | 10−5–10−6 | Yes | 117,118 |
PCB (pentaCB) | 10−7 | Yes | 104 |
FICZ | 10−10–10−12 | Yes | 109,119 |
Indirubin | 10−8 | Yes | 45,120 |
Lipoxin-4a | 10−9 | Yes | 121 |
Bilirubin | 10−6 | Yes | 122 |
ITE | 10−9 | ? | 123,124 |
ICZ | 10−8–10−10 | Yes | 116,125 |
This table contains some of the best studied AHR ligands. The EC50 is the dose of the ligand that leads to 50% of the maximal cytochrome P450 gene induction. These are estimates and are dependent on many factors, including cell type and AHR allele. Some AHR ligands are metabolized enzymatically and are short-lived. The EC50s of these ligands are sensitive to the timing of induction.
FICZ, 6-formylindolo(3,2-b)carbazole; ICZ, indolo(3,2-b)carbazole; ITE, 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester; PAH, polycyclic aromatic hydrocarbon; PCB, polychlorinated biphenyl; TCDD, 2,3,7,8 tetrachlorodibenzo-p-dioxin.