Drug (Charge of Major Microspecies at pH 7.4) Medical Application | IC50 [µM] | ||||||
---|---|---|---|---|---|---|---|
hOCT1 | hOCT2 | hOCT3 | hOCTN1 | hOCTN2 | hMATE1 | hMATE2-K | |
Abacavir (0) antiviral | 7 × 10−5 | 4 × 10−5 | 5 × 10−5 | ||||
Abemaciclib (+) antineoplastic | 1.5 | 0.52 | 0.75 | ||||
Adapalene (−) treatment of acne | <1 | ||||||
Alfuzosin (+) antiprostate hyperplasia | 15 | ||||||
Amodiaquine (+) antimalarial | 11 | ||||||
Amsacrine (+) antineoplastic | 5 | ||||||
Amitriptyline (+) antidepressant | 1.9–58 | 0.4–14 | >100 | ||||
Artemisin (0) antimalarial | 4.2 | ||||||
Atomoxetine (+) treatment of ADHS | 3.5–20 | ||||||
Atropine (+) mydriatic | 1.2, 12 | 1.3–29 | 446 | 5.9a | 53a | ||
Azidothymidine (+/−) antiviral | 0.0002 | 0.0003 | 0.0004 | ||||
Beclomethasone (0) antiasthmatic | 4.4 | ||||||
Benzethonium (+) antineoplastic | <1 | ||||||
Benztropine (+) anti-Parkinson | 0.3–13 | ||||||
Bithionol (−) anthelmintic | 2.2 | 1.9, <1 | 5.2a | 6.6a | |||
Bucindolol (+) vasodilatory | 15, 27 | ||||||
Budesonide (0) antiasthmatic | 7.3 | ||||||
Buflomedil (+) vasodilatory | n.t.d. | <1, n.t.d. | |||||
Buspirone (+) anxiolytic | 8.6–69 | 1.7a | 46a | ||||
Bisoprolol (+) antihypertensive | 2.4 | ||||||
Bosutinib (0) antichronic myeloic leukemia | 2.1 | ||||||
Camylofine (+) muscle relaxant | 9.1 | ||||||
Carbetapentane (+) antitussive | 1.6 | ||||||
Carvedilol (+) antihypertensive | 1.4, 3.4 | 2.3–63 | 74 | 73 | 124,a 146a | 79,a 131a | |
Cediranib (+) antineoplastic | 2.5 | ||||||
Chlorhexidine (++) antiseptic | 0.4 | 0.7a | 0.5a | ||||
Chlorphenesin (0) muscle relaxant | <1 | ||||||
Chlorpromazine (+) antipsychotic | 2.6–52 | 2.6, 14 | |||||
Clozapine (+) antidepressant | 1.8 | ||||||
Citalopram (+) antidepressant | 3, 19 | 12 | 145 | ||||
Clemastine (+) antiallergic | 4.9 | ||||||
Clomacran (+) sedative and hypnotic | <1 | ||||||
Clomipramine (+) antidepressant | 5, 19, n.t.d. | n.t.d. | |||||
Clonidine (+) sedative | 0.6–23, n.t.d. | 2–63, n.t.d. | 110, 373 | 8.1a | 54a | ||
Cloperastine (+) antitussive | 15 | ||||||
Closantel (−) antiparasitc | 3 | ||||||
Clotrimazole (0) antifungal | 12 | ||||||
Clozapine (+) antipsychotic | 1.8, n.t.d. | ||||||
Codeine (+) antitussive, analgesic | 11 | ||||||
Darunavir (0) antiviral | 16 | ||||||
Dasatinib (+) antineoplastic | 1.1 | 2.1 | 4.5 | 0.8a | 0.8a | ||
Des-fluoro (6)-quinolone (c.n.d.) antibiotic | 0.9, 1.3 | 0.8a | 0.1a | ||||
Dextromethorphan (+) antitussive | 10 | ||||||
Dichlorophene (−) antifungal | 8.4 | ||||||
Dicyclomine (+) antispasmodic | <1 | ||||||
Dipyramidole (0) antithrombotic | 81 | 2.6 | 26 | 74 | |||
Donepezil (+) anti-Alzheimer | 0.8a–1.5a | ||||||
Desipramine (+) antidepressant | 5–57 | 16 | 14 | 56a | 283a | ||
Dihydroergotamine (+) antimigraine | 50 | 2.8a | 13a | ||||
Dobutamine (+) treatment of heart failure | 4.2 | ||||||
Dolutegravir (0) antiviral | 0.07, 1.9 | >100 | 4.7a | >100a | |||
Domperidone (0) antemetic | 33 | 7.9 | 2.3a | 15a | |||
Doxazosin (+) antihypertensive | 15 | ||||||
Doxepin (+) antidepressant | 1.5, 12 | 0.25–13 | |||||
Eletriptan (0) antimigraine | 6.8 | ||||||
Epinastine (+) antiallergic | <1, 4.3 | 1.1a | 30a | ||||
Erlotinib (0) antineoplastic | 0.34, 16 | 5.2 | 4.2 | 3.8,a 7.9a | 3.5,a 6.2a | ||
Esmolol (+) treatment of tachycardia | 11a–25a | ||||||
Ethinylestradiol (0) contraceptive | 2.2 | 21a | 20a | ||||
Ethylacridinium (+) antiseptic | 0.08 | ||||||
Exemestane (0) treatment of breast cancer | <1 | ||||||
Fenfluramine (+) appetite suppressant | 10 | ||||||
Flecainide (+) antiarrhythmic | 2.5, 42 | 191, 234 | 60 | 176 | |||
Flurazepam (+) anticonvulsant | 53, 60 | ||||||
Gabexate (+) anticoagulant | 0.9 | 0.5a–0.70a | 11a | ||||
Gefitinib (0) antineoplastic | 1.1 | 24 | 5.5 | 1.8a | 0.19a | ||
Gentian violet (+) fungicidal | <1 | ||||||
Granisetron (+) antiemetic | 4.3 | 5.0a | 311a | ||||
Griseofulvin (0) antimycotic | 7.3 | ||||||
Guanabenz (+) antihypertensive | 4.9 | <1 | |||||
Guanfacine (+) antihypertensive | 3.5a | 218a | |||||
Imipramine (+) antidepressant | 6–37, n.t.d. | 0.4–6, n.t.d. | 42 | 42,a 10 | 183a | ||
Imiquimod (0) immune response modifier | 14a | 19a | |||||
Indinavir (0) antiviral | 37–208 | 142, 275 | >500 | 7.8a | >500a | ||
Irinotecan (+) antineoplastic | 1.4–21 | 0.31–16 | 75 | 7.9a | 79a | ||
Jatrorrhizine (+) promoting GI motility | 0.12, 0.82 | 0.18, 0.28 | |||||
Ketoconazole (0) antifungal | 2.6, 7.4 | 1.3a | 9.3a | ||||
Ketotifen (+) antiallergic | 13a–27a | ||||||
Lansoprazole (0) antacid | 36 | 3.3–9.5 | 3.1 | ||||
Leukomycin (+−) antibiotic | 182 | 11a | 125a | ||||
Mebeverine (+) antispasmodic | <1 | ||||||
Mefloquine (+) antimalarial | 6.6 | 15 | |||||
3,4-Methylenedioxymethamphetamine (+) stimulant | 24 | 1.6 | 74 | ||||
Mexiletine (+) antiarrhythmic | 19–50 | ||||||
Midazolam (0) hypnotic, anesthetic | 3.7 | ||||||
Mitoxantrone (++) antineoplastic | 44 | 73 | 61 | 0.5a; 4.4; 5.2 | 0.83a | ||
Nelfinavir (+) antiviral | 7, 22 | 13 | |||||
Nifekalant (++−) antiarrhythmic | >300 | 10.3 | 146 | 6.5a | 2.7a | ||
Nilotinib (0) antineoplastic | 2.9 | >30 | 0.35 | 3.4a | 1.8a | ||
Ondansetron (+) antiemetic | 0.3–64 | 0.2–16 | 1.7, 17 | 0.04a–4.0a, 0.15 | 0.03a–1.7,a 6.9 | ||
Olanzapine (+) antipsychotic | <1 | ||||||
Omeprazole (0) antacid | 16 | 6.7 | 22 | 16–24a | |||
Orphenadrine (+) muscle relaxant | 13, >100 | 2.5 | 65 | >100 | |||
Pantoprazole (0) treatment of gastric ulcera | 31, >500 | 0.56–2.8 | 23, 137 | 43a | >500a | ||
Phenoxybenzamine (+) antihypertensive | 2.7, 15 | 5 | 6 | ||||
Phentolamine (+) vasodilatory | 4.6a | 5.3a | |||||
Phenyltoloxamine (+) enhancer of analgetics | <1 | ||||||
Phenytoin (0) anticonvulsant | 0.75 | ||||||
Prochlorperazine (+) antipsychotic | 50, n.t.d. | n.t.d. | 7.9a–15a | ||||
Procyclidine (+) anti-Parkinson | <0.1 | ||||||
Proguanil (+) antimalarial | 13 | 4.4a | 1.4a | ||||
Promazine (+) antipsychotic | 17 | ||||||
Propafenone (+) antiarrhythmic | 1–16, n.t.d. | 3.6, 25, n.t.d. | 68 | ||||
Propantheline (+) treatment of hyperhidrosis | <1 | ||||||
Pyrimethamine (+) antimalarial | 8.5, 14 | 1.6–23 | 0.04a–1.2a, 0.08 | 0.01a–0.83,a 0.06 | |||
Quetiapine (0) antidepressant | 13 | ||||||
Rabeprazole (0) antacid | 3.0 | <1, 5.7 | 3.0 | ||||
Repaglinide (0) antidiabetic | 1.6, 9.2 | ||||||
Rapamycin (0) immune suppressive | 3.3, 3.5 | ||||||
Rimantadine (+) antiviral | 4.4 | 7.3a | 288a | ||||
Ritonavir (0) antiviral | 5–34 | 20, 25 | >100 | 1.3a–4.4a 14, 15 | 24,a 90a | ||
Rosiglitazone (−) antidiabetic | 6.9 | ||||||
Saquinavir (+) antiviral | 8, 37 | 205 | |||||
Scopolamine (0) antiemetic | 6.7, n.t.d. | 541, n.t.d. | 218 | 119a | 700a | ||
Sitagliptin (+) antidiabetic | 7.4 | ||||||
Sparteine (++) anticonvulsant, antiarrhythmic | <1 | ||||||
Spironolactone (0) antihypertensive | 1.2, 3 | 1.3 | 73 | 125 | 26, 36 | ||
Sulconazole (0) antifungal | <1 | ||||||
Sunitinib (+) antineoplastic | 0.33, 6.1 | 1.7 | 5.2 | 0.28a | 0.86 | ||
Tacrine (+) anti-Alzheimer | 22, 83 | 0.4–2.3 | 0.5a, 1.1 | 1.1,a >100 | |||
Tenatoprazole (0) antacid | 23 | 20 | 15 | ||||
Tenofovir disopoxil (0) antiviral | 9 × 10−5, >10 | 6 × 10−5 | 5 × 10−7 | ||||
Tetrachlorosalicylanilide (−) antiseptic | <1 | ||||||
Tolterodine (+) spasmolyticum | <1 | ||||||
Tramadol (+) | 18a | 75a | |||||
Trimipramine (+) antidepressant | 28 | 0.44 | |||||
Tripelenamine (+) antiallergic | 2.1–12 | ||||||
Tubocurarine (++) muscle relaxant | 79 | 9.4a | 56a | ||||
Valspodar (0), antidrug resistant | 2.0a–>15a | 0.11a–0.24a | |||||
Vecuronium (++) muscle relaxant | 3.5 | 1.9a | 25a | ||||
Zafirlukast (−) antiasthmatic | 9.7 | 4.3a | 7.6a | ||||
Ziprasidone (0) antidepressant | 3.6 | ||||||
Zolpidem (0) sedative, anticonvulsant | 0.15 |
c.n.d., charge not determined; GI, gastrointestinal; n.t.d., no transport detected under the employed experimental conditions.
↵a Uptake measurements performed in presence of an outwardly directed proton gradient.