Binding of pyridine and imidazole derivatives and benzphetamine to P450 2B6dH and L264F
Standard errors for fit to the respective equations are shown. The high-affinity ligands (4-NBP, 4-BP, 4-PI, and 4-CPI) were fit to the tight binding equation, whereas the low-affinity ligands (BEI, 1-BI, and BP) were fit to the Hill equation, as described under Materials and Methods. Results are representative of at least two independent determinations. The variation between the experiments is ≤10%.
Ligand | Ks | ||
|---|---|---|---|
| 2B6dH | L264F | ||
| μM | |||
| 4-(4-Nitrobenzyl)pyridine (4-NBP) | 0.07 ± 0.03 | 0.05 ± 0.03 | |
| 4-Benzylpyridine (4-BP) | 0.53 ± 0.19 | 0.62 ± 0.20 | |
| 4-Phenylimidazole (4-PI) | 0.10 ± 0.04 | 0.16 ± 0.05 | |
| 4-(4-Chlorophenyl)imidazole (4-CPI) | 0.87 ± 0.03 | 0.98 ± 0.04 | |
| 1-(2-Benzyloxy)ethyl) imidazole (BEI) | 2.06 ± 0.26 | 2.30 ± 0.92 | |
| 1-Benzylimidazole (1-BI) | 2.76 ± 0.14 | 4.31 ± 1.2 | |
| Benzphetamine (BP) | 52.5 ± 6.5a | 61.1 ± 6.6 | |
↵a Fit to Michaelis-Menten equation to derive Ks value.