Table II.
Comparison of Affinity for Human MATE1, MATE2-K, and OCT2 of Organic Cations and Various Drugs
| Compound | Affinity (Ki) for transporters (μM) | Plasma concentration (μM) | ||
|---|---|---|---|---|
| MATE1 | MATE2-K | OCT2 | ||
| Organic cation | ||||
| TEA | 380 (km)a | 760 (km)a | 48–270 | |
| MPP | 100 (km)a | 110 (km)a | 19–78 | |
| Guanidine | 2,100 | 4,200 | 3,030 | |
| Antidiabetic drug | ||||
| Metformin | 667 | 6,516 | 339–1,700 | 4.1 |
| Phenformin | 16 (IC50)b | 73 (IC50)b | 65 | Not used |
| Antiarrhythmic drug | ||||
| Disopyamide | 84 | 292 | 64 | >4.4 |
| Procainamide | 217 | 178 | 50–58 | 11–52 |
| Quinidine | 29 (IC50)b | 23 (IC50)b | 19 | 6–18 |
| Verapamil | 27.5 | 32.1 | 206 | 0.6 |
| Histamin H1 blocker | ||||
| Chlorpheniramine | 87.6 | 191.2 | 26 | 0.26 |
| Diphenhydramine | 87 | 266.5 | 32 | 0.9 |
| Histamin H2 blocker | ||||
| Cimetidine | 1.1 | 7.3 | 8.6–73 | 2.0–3.6 |
| Famotidine | 0.6 | 9.7 | 111–204 | 0.04 |
| Ranitidine | 25 | 25 | 40–265 | 0.28 |
| Antiparkinsonian drug | ||||
| Amantadine | 112 | 1,167 | 20–28 | 1.6 |
| Pramipexole | 141 | 24 | 17 | 0.001 |
| Antimalarial drug | ||||
| Quinine | 5 | 42 | 23–34 | 34 |
| Anticancer drug | ||||
| Cisplatin | 3,500 | >5,000 | 6,000 | 11 |
| Oxaliplatin | 4,000 | 1,000 | >5,000 | 0.83 |
Table II was modified from Tsuda et al. (38). The affinities (K m, K i, or IC50) for OCT2 were obtained from four different references (15,18,26,53). The affinities for MATE1 and MATE2-K (K m, K i, or IC50) were obtained from three references (32,33,38). The plasma concentrations were obtained from Thummel et al. (54)
a K m values were obtained from Tanihara et al. (32)
bIC50 values from Astorga et al. (33). Other K i values for MATE1 and MATE2-K were obtained from Tsuda et al. (38)