Preload | Uptake | Accumulation |
---|---|---|
nmol · mg−1 protein · min−1 | ||
None | Diphenhydramine | 34.7 ± 0.3 |
Chlorpheniramine | Diphenhydramine | 46.1 ± 0.42-150 |
None | Chlorpheniramine | 36.9 ± 0.8 |
Diphenhydramine | Chlorpheniramine | 48.0 ± 0.92-150 |
Caco-2 cells were preloaded for 30 min at 37°C with 1 mM chlorpheniramine or diphenhydramine (pH 7.4). After removing this medium, cell monolayers were washed once with ice-cold incubation medium and then incubated for 1 min at 37°C with 5 mM diphenhydramine or chlorpheniramine (pH 7.4). Thereafter, intracellular accumulation of drugs was measured. Each value represents the mean ± S.E. of three monolayers.
↵2-150 P < .01, significant difference from nonpreloaded value.