Concentrations (ng equivalent/ml) and percentage of total radioactivity (in parentheses) of vabicaserin and metabolites in plasma of male mice, rats, and dogs after a single oral administration
Concentrations were estimated based on the total plasma radioactivity concentrations and the percent distribution of plasma radioactivity.
| Species | Mice | Rats | Dogs | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Time (h) | 2 | 4 | 8 | 2 | 4 | 8 | 4 | 8 | 24 |
| Vabicaserin | 0.58 (15.1) | 0.46 (12.3) | 0.38 (11.7) | 86.9 (13.7) | 90.8 (13.8) | 58.7 (12.7) | 90.2 (16.0) | 4.75 (0.9) | 21.9 (1.6) |
| P1 | ND | ND | ND | 88.4 (14.0) | 59.7 (9.1) | 41.9 (8.9) | 36.4 (6.5) | 39.4 (7.5) | 68.3 (5.1) |
| P2 | 0.51 (13.4) | 0.55 (14.7) | 0.41 (12.7) | 32.3 (5.2) | 22.6 (3.4) | 20.0 (4.3) | 52.5 (9.3) | ND | 53.6 (4.0) |
| P3/M9 | 0.53 (13.8) | 0.57 (15.0) | 0.65 (19.8) | 76.4 (12.1) | 105 (16.0) | 64.2 (13.8) | 135 (24.0) | 364 (69.0) | 875 (65.3) |
| P4 | ND | ND | ND | 28.3 (4.4) | 28.3 (4.3) | 12.4 (2.5) | ND | ND | ND |
| P5 | ND | ND | ND | ND | ND | ND | 33.6 (6.0) | 7.04 (1.3) | ND |
| P7 | 0.25 (6.6) | 0.25 (6.5) | 0.19 (5.7) | 63.6 (10.1) | 62.1 (9.4) | 53.5 (11.5) | 41.5 (7.4) | ND | 88.0 (6.6) |
| P8 | ND | ND | ND | 15.1 (2.4) | 30.3 (4.6) | ND | ND | ND | ND |
| P10 | ND | ND | ND | 11.6 (1.9) | 14.2 (2.2) | 6.33 (1.4) | ND | ND | ND |
| P11 | ND | ND | ND | 23.7 (3.6) | 9.81 (1.5) | 13.2 (2.9) | ND | ND | ND |
| P12 | ND | ND | ND | 37.2 (6.0) | 34.5 (5.2) | 16.3 (3.6) | ND | ND | ND |
| P13 | ND | ND | ND | ND | ND | ND | 51.0 (9.1) | 27.5 (5.2) | ND |
| P14 | 0.3 (7.9) | 0.31 (8.2) | 0.26 (8.0) | ND | ND | ND | |||
| CG | 0.57 (14.9) | 0.78 (20.6) | 0.51 (15.7) | ND | ND | ND | 36.7 (6.5) | 12.3 (2.3) | 101 (7.5) |
| Othersa | 3.82 (28.3) | 3.77 (22.7) | 3.26 (26.5) | 168 (26.4) | 201 (31.0) | 179 (38.4) | 88.0 (15.6) | 72.0 (13.6) | 133 (9.9) |
ND, not detected.
↵a Sum of a number of uncharacterized minor metabolites, each representing less than 5% of plasma radioactivity.