TABLE 1

The apparent Ki values of various drugs for [14C]TEA uptake by hMATE1 and hMATE2-K

Each value represents the mean ± S.E. for three independent experiments.


Drug

Apparent Ki Values for [14C]TEA Uptake

Ratio of Ki Values (hMATE1/hMATE2-K)
hMATE1
hMATE2-K
μM
Antidiabetic drug
    Metformin 666.9 ± 30.2 6515.7 ± 792.4 0.10
Antiarrhythmic drugs
    Diltiazem 12.5 ± 0.7 117.0 ± 2.7* 0.11
    Disopyramide 83.8 ± 5.8 291.6 ± 38.3* 0.29
    Procainamide 217.0 ± 11.6 178.1 ± 19.3 1.22
    Quinidine 29.2 ± 3.1 23.1 ± 4.5 1.26
    Verapamil 27.5 ± 3.6 32.1 ± 4.4 0.85
Antidepressant drugs
    Desipramine 55.7 ± 14.5 283.0 ± 53.5* 0.19
    Imipramine 42.0 ± 9.0 182.9 ± 31.0* 0.23
Histamine H1 receptor antagonists
    Cetirizine 371.2 ± 42.7 817.6 ± 103.6* 0.45
    Chlorpheniramine 87.6 ± 8.5 191.2 ± 33.6* 0.46
    Diphenhydramine 87.0 ± 4.0 266.5 ± 53.4* 0.33
Histamine H2 receptor antagonists
    Cimetidine 1.1 ± 0.3 7.3 ± 0.7* 0.15
    Famotidine 0.6 ± 0.2 9.7 ± 0.4* 0.06
    Ranitidine 25.4 ± 2.1 25.0 ± 0.8 1.02
Antiparkinsonian agents
    Amantadine 111.8 ± 5.9 1167.0 ± 100.5* 0.10
    Pramipexole 141.4 ± 24.2 24.1 ± 3.4* 5.86
    Talipexole
66.0 ± 3.7
119.5 ± 15.3*
0.55
  • * P < 0.05, significantly different from the apparent Ki value of hMATE1.