Table 3

Relative distribution of radioactivity (%) among various peaks in the radiochromatographic profiles of pooled urine from rat, dog, and human following oral administration of [14C]omapatrilat

Metabolite3-a (Retention Time Range)Pooled Urine Samples (% Distribution)3-b
Rat (0–48 h)Dog (0–168 h)Human (0–168 h)
M1-a (13–14 min)251614
M1 (17–18 min)424
M2 (19–20 min)633225
M3 (26–27 min)3-c 78
M4 (28–29 min)3
M5 & M6 (30–32 min)14
M7(32–33 min)13
M8 (37–38 min)814
M1-c(44–46 min)1
M9 (51–52 min)1117
M10(57–58 min)15
Others3-d 455
Total3-e 979897
  • 3-a  Structures of metabolites are shown in Fig. 7 except for metabolite M10, which was identified as the symmetrical disulfide of omapatrilat.

  • 3-b  Radioactive peaks are reported as a percentage of the total radioactivity eluted from the column after background subtraction. The recovery of the radioactivity from the column was quantitative.

  • 3-c  Percentages less than 1% are not reported.

  • 3-d  Radioactivity from peaks that have not been identified.

  • 3-e  Total is less than 100% because remainder of the radioactivity is distributed in small amounts (<0.5%) in various fractions throughout the radiochromatogram.