TABLE 2

IC50 values for inhibition of MPP+ (10 μM) uptake mediated by OCT2 p.270Ala>Ser mutant protein compared with wild-type OCT2

Each value represents the mean and the 95% confidence interval of 6 to 9 determinations from 2 to 3 independent experiments.


Drug

OCT Wild-Type

OCT2 p0.270Ala>Ser

p
IC50
95% CI
IC50
95% CI
μM μM
Amitriptyline 14 11-19 13 9-18
Carvedilol 63 27-149 33 16-67
Chloroquine 1087 604-1955 926 552-1553
Chlorpromazine 14 11-18 19 13-26
Cimetidine 126 91-176 422 316-564 0.0046
Clonidine 16 12-22 20 15-29
Desloratadine 60 48-76 62 47-81
Diphenhydramine 21 14-31 21 13-34
Disopyramide 325 209-504 132 122-440
Dopamine 3485 1683-7216 3325 2038-5425
Doxepin 13 6-27 16 9-29
Fenfluramine 10 5-19 16 7-33
Flecainide 191 77-470 264 141-494
Flurazepam 53 36-78 110 79-154 0.0167
Imipramine 6 4-8 9 6-13
Ipratropium bromide 15 9-25 16 10-28
Levomethadone 60 33-108 94 53-167
Mefloquine 204 136-306 188 93-382
Metformin 397 300-526 936 753-1163 0.0006
Mexiletine 42 32-54 78 55-114 0.0198
Propafenone 25 16-39 17 11-27
Propranolol 189 117-304 895 543-1473 0.0008
Quinidine 87 46-164 51 32-81
Sibutramine 29 16-52 16 9-29
Tamoxifen 87 37-205 92 26-331
Trimethoprim 1327 725-2430 1001 698-1436
Verapamil
70
60-82
120
87-165
0.0098