Table 4 Activation of mouse, rat, rabbit, and chicken PXRs
From: Evolution of pharmacologic specificity in the pregnane X receptor
Cmp # | Compound | Mouse PXR Activity (efficacy, ε, in parentheses) | Rat PXR Activity (efficacy, ε, in parentheses) | Rabbit PXR Activity (efficacy, ε, in parentheses) | Chicken PXR Activity (efficacy, ε, in parentheses) |
|---|---|---|---|---|---|
BI004 | Murideoxycholic acid | 5.09 (ε = 0.76) | 4.80 (ε = 0.22) | 4.52 (ε = 1.86) | No effect |
BI005 | Chenodeoxycholic acid | No effect | No effect | 4.70 (ε = 0.42) | 4.70 (ε = 0.36) |
BI008 | Deoxycholic acid | No effect | 5.00 (ε = 0.32) | 4.44 (ε = 0.37) | No effect |
BI011 | Lithocholic acid | 4.86 (ε = 0.48) | 4.78 (ε = 0.42) | 4.80 (ε = 0.70) | 5.09 (ε = 0.17) |
BI020 | Cholic acid | No effect | 4.82 (ε = 0.42) | 4.02 (ε = 0.67) | 4.47 (ε = 0.36) |
BI023 | 5β-Cholestan-3α,7α,12α-triol | 5.85 (ε = 1.23) | 5.65 (ε = 0.72) | 5.41 (ε = 0.37) | 5.89 (ε = 0.27) |
BI034 | 5β-Scymnol sulfate | 4.44 (ε = 0.85) | 4.40 (ε = 0.85) | 4.09 (ε = 1.93) | 4.37 (ε = 0.88) |
BI036 | 5α-Cyprinol sulfate | 4.78 (ε = 0.29) | 4.50 (ε = 0.28) | 4.09 (ε = 0.43) | 4.51 (ε = 0.61) |
BI038 | 3α,7α,12αtTrihydroxy-5β-cholestan-27-oic acid, taurine conjugated | No effect | No effect | No effect | No effect |
BI046 | Tauro-β-muricholic acid | No effect | No effect | No effect | No effect |
BI047 | 7α-Hydroxycholesterol | No effect | No effect | No effect | No effect |
PR2 | 5β-Pregnane-3,20-dione | 5.36 (ε = 0.84) | 5.24 (ε = 1.01) | 4.90 (ε = 1.0) | 5.59 (ε = 0.81) |
MI3 | Benzo [a]pyren | 4.86 (ε = 0.94) | 4.85 (ε = 0.45) | No effect | 4.40 (ε = 0.50) |
MI4 | n -Butyl- p -aminobenzoate | No effect | < 4 | < 4 | > 100 |
MI22 | Nifedipine | 4.64 (ε = 0.51) | 5.26 (ε = 0.68) | 4.61 (ε = 0.29) | 6.14 (ε = 1.00) |
MI34 | TCDD (2,3,7,8-tetrachlorodienzo- p -dioxin) | 7.00 (ε = 1.60) | 6.70 (ε = 0.83) | No effect | 7.04 (ε = 0.06) |
AN1 | 5α-Androstan-3α-,17β-diol |  |  |  | 5.07 (ε = 2.28) |
AN3 | 5α-Androstan-3α-ol |  |  |  | 5.38 (ε = 0.85) |
AN21 | 5α-Androst-16-en-3β-ol |  |  |  | 5.14 (ε = 2.99) |
AN22 | 5α-Androst-16-en-3-one |  |  |  | 4.99 (ε = 0.77) |
BI031 | Allocholic acid | Â | Â | Â | No effect |
BI006 | Glycochenodeoxycholic acid |  |  |  | 4.60 (ε = 0.41) |
BI007 | Taurochenodeoxycholic acid | Â | Â | Â | No effect |
BI009 | Glycodeoxycholic acid |  |  | 4.81 (ε = 0.40) |  |
BI010 | Taurodeoxycholic acid |  |  | 4.84 (ε = 0.15) |  |
BI017 | ω-Muricholic acid | No effect | No effect |  |  |
BI018 | α-Muricholic acid | 4.59 (ε = 2.63) | 3.95 (ε = 1.31) |  |  |
BI019 | β-Muricholic acid | No effect | No effect |  |  |
BI021 | Glycocholic acid | No effect | No effect | Â | No effect |
BI022 | Taurocholic acid | 4.07 (ε = 0.93) | No effect |  | No effect |
BI042 | 7-Ketodeoxycholic acid |  |  | 4.31 (ε = 1.55) |  |
PR13 | Pregenolone 16α-carbonitrile | 6.41 (ε = 1.0) | 6.20 (ε = 1.0) |  |  |