Table 1.
Inhibitory effects (mean ± average deviation (AD)) of various drugs on hOCT2- and mOct2-mediated metformin-uptake. * Decynium22 is a control inhibitor for OCTs.
| Drugs/Pos. Control Inhibitor * | Type of Drug | Charge at pH 7.4 | Inhibitory Effects (%) | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| hOCT2 | mOct2 | |||||||||
| 10 µM | 100 µM | 10 µM | 100 µM | |||||||
| Mean | AD | Mean | AD | Mean | AD | Mean | AD | |||
| Zosuquidar | antineoplastic drug | 37% uncharged 63% cation | −10 | 5 | −47 | 11 | −11 | 10 | −30 | 7 |
| Procainamid | class I antiarrhythmic agent | 100% cation | −20 | 9 | −44 | 14 | −16 | 3 | −30 | 0 |
| Ritonavir | antiretroviral HIV | 100% cation | −10 | 13 | −38 | 12 | 1 | 4 | −8 | 1 |
| Ranitidine | H2 histamine receptor antagonist | 100% cation | −43 | 18 | −33 | 30 | −37 | 12 | −16 | 11 |
| Quinidine | class I antiarrhythmic agent | 100% cation | −50 | 14 | −31 | 9 | −38 | 11 | −28 | 3 |
| Amiodarone | class III antiarrhythmic agent | 100% cation | −10 | 17 | −27 | 12 | −7 | 0 | 4 | 12 |
| Reserpine | hypertension | 70% uncharged 30% cation | −13 | 7 | −27 | 1 | −27 | 11 | −19 | 7 |
| Cimetidine | H2 histamine receptor antagonist | 75% uncharged 25% cation | −50 | 25 | −17 | 4 | −42 | 2 | 24 | 6 |
| CyclosporinA | immunsuppressant | 100% cation | −8 | 1 | 0 | 4 | −13 | 11 | −5 | 9 |
| Verapamil | class IV antiarrhythmic agent | 100% cation | −8 | 2 | 44 | 18 | 23 | 6 | 73 | 0 |
| Elacridar | bioenhancer targeting drug resistance in tumors | 100% cation | 25 | 5 | 65 | 0 | 56 | 14 | 81 | 2 |
| Clonidine | hypertension | 100% cation | 40 | 0 | 76 | 6 | 54 | 1 | 89 | 3 |
| Ketoconazole | antifungal | 82% uncharged 18% cation | 31 | 9 | 87 | 2 | 49 | 1 | 87 | 3 |
| Decynium22 * | inhibitor for cation transporter | 100% cation | 67 | 8 | 96 | 0 | 72 | 1 | 97 | 0 |