TABLE 1

Digoxin uptake methodologies

Expression SystemOATPs InvestigatedDigoxin Uptake ExperimentsPositive Controls/Inhibitors/Negative Controls
Digoxin ConcentrationUptake TimeTemperatureControl SubstrateUptake TimeUptake InhibitorNegative Control
μM°C
GSKHEK293 cells transduced with recombinant BacMam virusOATP1B10.01, 0.05, 0.25, 0.5, 5, and 503 min370.02 μM E17βG3 minRifamycin
OATP1B310 min0.02 μM E17βG10 minRifamycin
OATP1A230 s0.02 μM E3S30 sKetoconazole
OATP2B130 s0.02 μM E3S30 sMontelukast
BIHEK293 and CHO cells transiently transfected with transporter containing plasmid DNAOATP1B31371 μM CCK-810 minRifamycin
OATP2B10.5 μM EE3S3 minRifamycinHEK293 and CHO cells transiently transfected with control DNA
PfizerStably transfected HEK293 cellsOATP1B11 & 104 min375 μM E17βG4 minRifamycinUntransfected HEK293 cells
OATP1B35 μM E17βGRifamycin
OATP2B15 μM UK191005
SolvoCHO cellsOATP1B11.2 & 1115 min370.1 μM E3S15 minCerivastatin
CHO cellsOATP1B30.1 μM E3SFluvastatin
MDCKII cellsOATP2B110 μM Fluo-3Fluvastatin
  • E3S, estrone 3-sulfate; E17βG, estradiol-17β-d-glucuronide; CCK-8, cholecystokinin-8.