TABLE 1

Model substrates of human organic cation transporters

Charge of major microspecies at pH 7.4 was calculated with program MarvinSketch version 19.3 of ChemAxon (https://chemaxon.com/products/marvin). ASP: Biermann et al., 2006; Grigat et al., 2009; Ahlin et al., 2011; Kido et al., 2011; Wittwer et al., 2013; Chen et al., 2017a; Sandoval et al., 2018, DAPI (4′,6-diamidino-2-phenylindole): Yasujima et al., 2010, 2011, fluoro-L-α-methyltyrosine: Wei et al., 2016, fluoromethylcholine: Visentin et al., 2017b, 2018, MPP: Gorboulev et al., 1997; Zhang et al., 1997; Ohashi et al., 1999; Wu et al., 2000; Bednarczyk et al., 2003; Gründemann et al., 2003; Otsuka et al., 2005; Sata et al., 2005; Masuda et al., 2006; Tanihara et al., 2007; Lee et al., 2009; Zolk et al., 2009a; Astorga et al., 2012; Belzer et al., 2013; Bexten et al., 2015; Lechner et al., 2016; Martínez-Guerrero et al., 2016, NBD-MTMA: Belzer et al., 2013; Martínez-Guerrero and Wright, 2013; Martínez-Guerrero et al., 2016; Sandoval et al., 2018, N-metyl-quinidine: Van Montfoort et al., 2001, rhodamine 123: Jouan et al., 2014; Lechner et al., 2016, TEA: Gorboulev et al., 1997; Zhang et al., 1997; Tamai et al., 1998; Ohashi et al., 2002; Bednarczyk et al., 2003; Peltekova et al., 2004; Bourdet et al., 2005; Otsuka et al., 2005; Masuda et al., 2006; Geier et al., 2007; Tanihara et al., 2007; Umehara et al., 2007; Cheng et al., 2009; Ming et al., 2009; Ohta et al., 2009; Astorga et al., 2012; Belzer et al., 2013; Hendrickx et al., 2013; Sandoval et al., 2018.

Compound (Charge of Major Microspecies at pH 7.4)Apparent Km (IC50) [µM]
hOCT1hOCT2hOCT3hOCTN1hOCTN2hMATE1hMATE2-K
ASP (+) f2.3–2136–42n.t.d.5.8a, 34a
DAPI (++) f8.9n.t.d.n.t.d.n.t.d.n.t.d.1.1a3.2a
Fluoro-L-α-methyltyrosine (+−)n.t.d.n.t.d.t
Fluoromethylcholine (+)t14, 1800t
MPP (+)15–32 (16)3–20 (3.0)47–83n.t.d.4.4a–100a (22a–54a)3.3a–111a
NBD-MTMA (++) f8.8, 9.6 (8.3, 64)20,a 105a (67a–112a)
N-methyl-quinindine (+)20
Rhodamine 123 (+) f0.54 (0.37)0.61 (62)0.79a10a
TEA (+)69–229 (216)27–76 (110, 222)(1240–1480)439292, 304220,a 380a (41a)760,a 830a (14a)
  • f, fluorescent; NBD-MTMA, N,N,N-trimethyl-2-[methyl(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)amino]ethanaminium iodide; n.t.d., no transport detected; t, transported.

  • a Uptake measurements performed in presence of an outwardly directed proton gradient; IC50 values are presented in brackets.