Compound (Charge of Major Microspecies at pH 7.4) | Km (IC50) [µM] | ||||||
---|---|---|---|---|---|---|---|
hOCT1 | hOCT2 | hOCT3 | hOCTN1 | hOCTN2 | hMATE1 | hMATE2-K | |
Acetylcholine (+) | (580) | 117 | 1000 | ||||
Acetyl-L-carnitine (+/−) | 8.5 | ||||||
Agmatine (++) | t (24,000) | 1400 | 2500 | (54a) | (61a) | ||
Betaine (+/−) | t | t | |||||
Choline (+) | t (3540) | 210–404 | t (231) | t (>2000) | (>5000a) | ||
Creatinine (+) | t | 1820, 4000 (580) | 1320 | n.t.d. | n.t.d. | >2000 (195a) | >2000 (150a) |
Cyclo (His-Pro) (0) | 655 | 74 | 126 | ||||
D-Carnitine (+/−) | 11, 98 | ||||||
L-Carnitine (+/−) | 571 | 3.5–7.7 | n.t.d. | ||||
2′Deoxycytidine (0) | t | ||||||
Dopamine (+) | t (487) | 390–1400 | 800. | ||||
Epinephrine (+) | t | 420 | 240 | ||||
Ergothioneine (+/−) | 21, 85 | n.t.d. | |||||
Estrone 3-sulfate (−) | 470a | 850a | |||||
Guanidine (+) | (2200, 3030) | (6201) | n.t.d., n.i.d. | 2100a | 4200a | ||
6-β-Hydroxycortisol (0) | t | t | |||||
Histamine (+) | t (3007) | 940, 1300 | 180, 220 | (761a) | (775a) | ||
Lysine (++/−) | t | ||||||
Methionine (+/−) | t | ||||||
N-1-methylnicotinamide (0) | (1035, 7700) | 318 (266–1000) | (77) | i.n.f.t. | 301 | 422 | |
Norepinephrine (+) | t | 1500–5450 | 182–2630 | ||||
Salsolinol (+) | 440 | 130 | 139 | ||||
Serotonin (+) | 197 (>20,000) | 80, 290 | 900 (1000) | (29a) | (18a) | ||
Stachydrine (+/−) | 270 | ||||||
Thiamine (+) | 780 (434) | 60, 750 | t | 3.5a,b, 31 | 3.9a,b, 23 | ||
Trimethylamine-N-oxide (+/−) | 33,900 | 7370, 74,000 | n.t.d. | ||||
Tyramine (+) | t (107) | t | (87a) | (138a) | |||
Quercetin (0) | t |
i.n.f.t., inhibition, not tested for transport; n.i.d., no inhibition detected; n.t.d., no transport detected; t, transported.
↵a Uptake measurements performed in presence of an outwardly directed proton gradient.
↵b Determination of the low apparent Km values is supposed to be due to the fact that only thiamine concentrations up to 100 µM were tested and the Km of an apparent high-affinity transport site was obtained.