Characterization of transport in isolated human hepatocytes: A study with the bile acid taurocholic acid, the uncharged ouabain and the organic cations vecuronium and rocuronium
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Cited by (67)
Electrophysiological characterization of human Na<sup>+</sup>/taurocholate cotransporting polypeptide (hNTCP) heterologously expressed in Xenopus laevis oocytes
2014, Archives of Biochemistry and BiophysicsCitation Excerpt :NTCP is predominantly expressed at the basolateral membrane in the liver and is mostly involved in Na+-dependent uptake of bile acids from the portal blood circulation. To date, the Na+-dependent uptake via hNTCP has been corroborated by various experimental systems with isolated perfused liver [45], isolated hepatocytes [20,23,24,46], isolated membrane vesicles [47] and hNTCP expressed in mammalian cultured cells [15–17] or heterologously in X. laevis oocytes [22,43]. As far as we are aware, however, there is no direct evidence for the electrogenic nature of bile acid transport via hNTCP.
The SLC10 carrier family: Transport functions and molecular structure
2012, Current Topics in MembranesCitation Excerpt :In the human hepatocyte cell model, the apparent kinetic parameters of affinity (Km) and capacity (Vmax) for TC uptake differed from data of rat Ntcp. A direct comparison of both species showed that in human hepatocytes, the Km was 2–3 times higher (Sandker et al., 1994) or quite similar (Azer & Stacey, 1993) but Vmax was consistently much lower than for TC transport in rat hepatocytes (e.g. Vmax 300 pmol/min/106 human cells versus 1800 pmol/min/106 rat cells), reflecting less-efficient uptake of the BS in human hepatocytes (Azer & Stacey, 1993; Sandker et al., 1994). In NTCP transfected cells such as HeLa cell, COS cells as well as in X. laevis oocytes Km for TC transport was, however, always lower (Table 1) than in human hepatocytes (Hagenbuch & Meier, 1994; Kim et al., 1999), reflecting higher affinity in transfected cell systems.
Sodium fluorescein is a probe substrate for hepatic drug transport mediated by OATP1B1 and OATP1B3
2011, Journal of Pharmaceutical SciencesCitation Excerpt :However, the Vmax for NaFluo in rat hepatocytes was approximately 13‐fold higher relative to human hepatocytes. Several fold higher Vmax values in rat versus human hepatocytes have previously been reported for TC, EG, ouabain, and the two short acting muscle relaxants vecuronium and rocuronium.29,35 The uptake of NaFluo was examined in presence and absence of sodium to determine the possible contribution of sodium‐dependent uptake by Ntcp/NTCP in rat and human hepatocytes (Figure 2a and 2c).
Determination of OATP-, NTCP- and OCT-mediated substrate uptake activities in individual and pooled batches of cryopreserved human hepatocytes
2011, European Journal of Pharmaceutical SciencesCitation Excerpt :As there are interspecies-differences in drug metabolizing enzymes and in the substrate affinity profiles of transporters (Ishizuka et al., 1999; Ye et al., 2010), hepatocytes of human origin are required to make relevant extrapolations from in vitro drug transport data towards the in vivo situation in human. A few studies have been conducted illustrating the feasibility of plated and suspended human hepatocytes to study hepatic drug transport activities (Sandker et al., 1994; Olinga et al., 1998; Shitara et al., 2003; Yamashiro et al., 2006; Bi et al., 2006). However, the chronic limitation in availability of freshly-isolated human hepatocytes may have precluded more systematic studies on transporter activities in these cells.
Inhibition of Na<sup>+</sup>-taurocholate co-transporting polypeptide-mediated bile acid transport by cholestatic sulfated progesterone metabolites
2010, Journal of Biological ChemistryCitation Excerpt :The IC50 and Ki values for the P4-S compounds studied are similar to the total levels of PM4-S + PM5-S observed in third trimester pregnant serum (6.2 μm; Fig. 6) and within the documented total P4-S levels in the serum of ICP patients (21), typifying the physiological importance of pregnancy levels of P4-S in women with raised serum bile acid levels. In agreement with previous reports (35), our study has revealed that Na+-dependent uptake is responsible for the majority of temperature-sensitive bile acid influx into the hepatocyte that is mediated by the NTCP transporter (Fig. 1C). We showed that PM4-S and PM5-S significantly inhibit Na+-dependent bile acid uptake (Table 1 and Fig. 3, B and C).
Function of Uptake Transporters for Taurocholate and Estradiol 17b-D-Glucuronide in Cryopreserved Human Hepatocytes
2003, Drug Metabolism and Pharmacokinetics