TABLE 1

IC50 values for inhibitors of metformin uptake via cation-selective transporters

The IC50 values reported were experimentally determined except for those entries in which literature values are cited.

InhibitorIC50 Values (Mean ± S.D.)
OCT1OCT2OCT3SERTCHTCTLs
µM
Mitoxantrone3.0 ± 0.8135.0 ± 12.0174.0 ± 19.0977.2 ± 1.2N/AN/A
Cimetidine20.9 ± 1.416.6 ± 1.39.8 ± 1.3N/AN/AN/A
Corticosterone3.2 ± 0.51.3 ± 0.10.2 ± 0.1N/AN/AN/A
Paroxetine1.0 ± 0.211.9 ± 1.26.4 ± 1.30.0060 ± 0.00059N/AN/A
Desipramine2.2 ± 0.42.4 ± 0.23.8 ± 0.30.054 ± 0.0042aN/AN/A
HC3112.2 ± 1.5131.8 ± 1.4524.8 ± 1.770.8 ± 1.20.004b~100c
  • N/A, not available.

  • a Barker et al., 1994.

  • b Apparsundaram et al., 2000.

  • c Lockman and Allen, 2002.