TABLE 4

Plasma concentrations of total radioactivity, vabicaserin, and CG (ng equivalents/ml) in mice, rats, and dogs after a single oral administration of [14C]vabicaserina

TimeMouseRatDog
TotalVabicaserinCGTotalVabicaserinCGTotalVabicaserinCG
h50 mg/kg, n = 4–55 mg/kg, n = 315 mg/kg, n = 2–3
Male
    23819 ± 622582 ± 173582 ± 199632 ± 14487 ± 35N.D.422 ± 57331120
    43771 ± 512475 ± 177773 ± 293659 ± 1791 ± 23N.D.564 ± 748199108
    83263 ± 624385 ± 135491 ± 116465 ± 4359 ± 16N.D.528 ± 5665 ± 813 ± 22
    24597 ± 21324 ± 16213 ± 11947 ± 8N.A.N.A.1340 ± 50828 ± 24107 ± 135
AUC0–24b56,357663110,09782671037N.D.18,5369331550
Female
    25250 ± 583999 ± 181344 ± 157658 ± 189132 ± 61N.D.N.A.N.A.N.A.
    82868 ± 615356 ± 135375 ± 183338 ± 6149 ± 13N.D.N.A.N.A.N.A.
  • N.D., not detected; N.A., data not available.

  • a Data are presented as mean ± S.D. or the average of two subjects.

  • b AUC0–24 values were calculated with mean plasma concentrations using WinNonlin 5.1 (Pharsight) and were presented as ng-Eq · h/ml.