TABLE 2

Cimetidine inhibition constants for the renal organic cation transporters

Data shown in Fig. 2 and 5 were used to determine these Ki values calculated by using nonlinear regression analysis as described under Materials and Methods. Each parameter represents the mean value ± computer-calculated S.D.

Inhibition Constant (Ki)
TEAMetforminMPP+ASPMIBG
μM
OCT1155 ± 27104 ± 23223 ± 34186 ± 13101 ± 13
OCT2144 ± 25124 ± 20146 ± 32104 ± 1095 ± 16
Oct199 ± 1354 ± 1555 ± 667 ± 1394 ± 18
Oct2122 ± 2461 ± 13143 ± 3271 ± 1084 ± 14
MATE11.1 ± 0.33.8 ± 0.82.7 ± 0.52.9 ± 0.31.7 ± 0.3
MATE2-K2.1 ± 0.56.9 ± 2.34.0 ± 0.82.5 ± 0.32.7 ± 0.3
mMate11.4 ± 0.43.6 ± 0.73.0 ± 0.82.6 ± 0.42.0 ± 0.5