Molar balance of pimozide metabolism in pooled HLMs

Mean (S.D.) amounts (picomoles) of pimozide molecules depleted and pimozide metabolites formed by pooled (n = 200 donors) human liver microsomes incubated with pimozide (10 pmol starting amount, 50 nM starting concentration) for 20 min. Percentage standardization of metabolites formed relative to pimozide molecules depleted is also provided.

5-Hydroxypimozide6-HydroxypimozideDHPBISum of MetabolitesaPimozide Depletedb
Amount (pmol)0.27 (0.040)0.11 (0.035)2.4 (0.20)2.8 (0.17)3.1 (0.80)
% Depleted Accountedc8.7 (1.3)3.5 (1.1)78 (6.5)90 (5.5)N/A
  • N/A, not applicable.

  • a Denotes sum of amounts of DHPBI, 5-hydroxypimozide, and 6-hydroxypimozide formed during each incubation.

  • b Denotes the difference between pimozide amounts measured at time 0 and 20 min in each incubation.

  • c Sum of metabolite amounts divided by amount of pimozide depleted over the course of the incubation, expressed as a percentage (see eq. 1).