TABLE 2

Comparison of affinity for hMATE1, hMATE2-K, and hOCT2 (rOCT2) of organic cations and various drugs excreted from kidney


Compounds

Km or Ki Values for [14C]TEA Uptake

Affinity for hOCT2 (rOCT2) from Previous Articlesb

Comparison of Affinity

Effective Plasma Concentrationc
hMATE1
hMATE2-K
μM μM
Organic cations
    TEA 380a 760a 48-270 MATE < OCT
    1-Methyl-4-phenylpyridinium 100a 110a 19-78 MATE < OCT
Antidiabetic drug
    Metformin 667 6516 339-1700 MATE < OCT 4.1
Antiarrhythmic drugs
    Disopyramide 84 292 (64) MATE < OCT >4.4
    Procainamide 217 178 50-58 MATE < OCT 11-52
    Quinidine 29 23 (19) MATE < OCT 6-18
Histamine H1 receptor antagonist
    Cetirizine 371 818 No data 0.55
Histamine H2 receptor antagonists
    Cimetidine 1.1 7.3 8.6-73 MATE > OCT 2.0-3.6
    Famotidine 0.6 9.7 111-204 MATE > OCT 0.04
    Ranitidine 25 25 40-265 MATE > OCT 0.28
Antiparkinsonian agents
    Amantadine 112 1167 20-28 MATE < OCT 1.6
    Pramipexole 141 24 (17) MATE < OCT 0.001
    Talipexole
66
120
No data

0.002