TABLE 3.
Overview of clinically relevant drugs that are orally administered and potent inhibitors of OCT1.
| Drug/compound | Class | Inhibitory effect | References |
|---|---|---|---|
| Amitriptyline | Non-selective NSRI | IC50 = 4.4 µM | Tzvetkov et al. (2013) |
| Cimetidine | H2-receptor antagonist | IC50 = 60 µM | Koepsell (2020) |
| Citalopram | SSRI | IC50 = 2.8 µM | Koepsell et al. (2007) |
| Clonidine | α-adrenoceptor antagonist | IC50 = 0.6–6.5 µM | Koepsell et al. (2007) |
| Desipramine | Non-selective NSRI | IC50 = 5.4 µM | Koepsell et al. (2007) |
| Diphenhydramine | H1-receptor antagonist | IC50 = 3.4 µM | Müller et al. (2005) |
| Fluoxetine | SSRI | IC50 = 6.0 µM | Tzvetkov et al. (2013) |
| Imipramine | Non-selective NSRI | IC50 = 6.2 µM | Tzvetkov et al. (2013) |
| Memantine | NMDA receptor antagonist | IC50 = 3.7 µM | Busch et al. (1998) |
| Metoclopramide | D2/5-HT3 receptor anatgonist | IC50 = 16–95 µM | Koepsell (2020) |
| Morphine | Opioid receptor agonist | IC50 = 4.2–28 µM | Koepsell (2020) |
| Ondansetron | 5-HT3 receptor antagonist | IC50 = 1.2 µM | Tzvetkov et al. (2013) |
| Oxybutynin | Muscarinic receptor antagonist | IC50 = 20 µM | Koepsell (2020) |
| Prazosin | α-adrenoceptor antagonist | IC50 = 1.8 µM | Hayer-Zillgen et al. (2002) |
| Quinidine | Na+channel blocker (antiarrhythmic) | IC50 = 18 µM | Koepsell et al. (2007) |
| Quinine | Antimalaria drug | IC50 = 13–23 µM | Koepsell et al. (2007) |
| Ranitidine | H1-receptor antagonist | IC50 = 28 µM | Müller et al. (2005) |
| Ritonavir | HIV protease inhibitor | IC50 = 5.2 µM | Zhang et al. (2000) |
| Trospium | Muscarinic receptor antagonist | IC50 = 5.3–18 µM | Koepsell (2020) |
| Verapamil | Ca2+channel blocker | IC50 = 1.6–2.9 µM | Koepsell et al. (2007), Tzvetkov et al. (2013) |
IC50, half maximal inhibitory concentration; NMDA, N-methyl-D-aspartate; NSRI, norepinephrine and serotonin reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor.