Table 9

Category IIA: nontransported substrates (NYY)

Compound NamePapp A → BMass Balance A → BPapp B → AMass Balance B → ABA/AB RatioEffluxed (Y/N)ATPase Assay RatioATPase Activator (Y/N)Calcein-AM AssayCalcein-AM Inhibitor (Y/N)
nm/s nm/s % max
BW 1136U89355  ± 17.462.0434  ± 38.176.31.22N6.34Y79.2Y
BW 565C81405  ± 26.875.6504  ± 30.990.21.24N4.92Y56.3Y
Chlorpromazine438  ± 42.764.1477  ± 57.278.41.09N2.42Y30.4Y
Ketoconazole316  ± 11.750.7323  ± 23.149.21.02N9-a 7.44Y73.4Y
Mebendazole714  ± 11392.0648  ± 58.988.20.91N9-b 2.00Y38.6Y
Midazolam701  ± 48.7101564  ± 8.7895.60.81N9-b 3.82Y74.9Y
Nicardipine614  ± 90.997.7661  ± 15.61161.08N9-b 5.39Y102Y
Nifedipine610  ± 81.1105765  ± 71.81261.26N2.08Y34.8Y
Nitrendipine604  ± 53.890.9483  ± 28.91100.8N3.22Y48.3Y
Verapamil591  ± 59.6107687  ± 13.598.91.16N7.64Y56.4Y
 Mean5355551.064.5359.4
 Median5985341.094.3756.4
 Minimum3163230.8230.4
 Maximum7147651.267.64102

n = 10 compounds.

  • Y, yes; N, no; BW, Burroughs Wellcome compounds, which are a series of acrivastine derivatives (Christensen et al., 1997).

  • 9-a  Run twice with the results and mass balances similar between experiments.

  • 9-b  Run in the presence and absence of 2 μM GF120918 to confirm whether the compound is transported by Pgp.