Table 7.
Caco-2 Cell Permeability and CYP450 Isoform Inhibition of Compound 22
compd |
Papp (nm/s)a
|
CYP450 isoform (% inhibition at 1 μM)
|
|||||
---|---|---|---|---|---|---|---|
PA→B | PB→A | CYP1A2 | CYP2C19 | CYP2C9 | CYP2D6 | CYP3A4 | |
22 | 123.2 | 107.3 | 66.8 | 72.6 | 28.9 | <5.0 | 12.2 |
Papp (nm/s): >50, high; 10–50, medium; <10, low; caffeine PA–B reference control, 206 ± 35 nm/s; cimetidine PA–B and PB–A reference control, 1.1 ± 0.1 and 21.3 ± 3.4 nm/s, respectively.