From: Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
Nor-BNI | GNTI | JDTic | |||
---|---|---|---|---|---|
t max | h | 0.5 | 0.5 | 0.5 | |
C max,p | ng mL-1 | 4,025 | 3,080 | 245 | |
C max,brain | ng mL-1 | 443 | < 120 | 71 | |
C max,brain,u | nmol L-1 | < 26 | < 6 | < 4 | |
AUC 0–∞,p | ng h mL-1 | 6,422 | 9,486 | 888 | |
AUC 0–∞,brain | ng h mL-1 | 593 | - | 10,304 | |
V z /F | L kg-1 | 19 | 4.4 | 83 | |
CL/F | L kg-1 h-1 | 1.7 | 1.0 | 1.1 | |
AUC0 –∞,brain /AUC0 –∞,p | K p,brain | 0.09 | – | 11.6 | |
AUC 0–∞,brain,u /AUC 0–∞,p,u | K p,uu,brain | < 0.007 | – | < 1.4 | |
C max,brain /C max,p | 0.11 | 0.0085a | 0.29 | ||
C max,brain,u /C max,p,u | < 0.009 | < 0.0007a | < 0.04 |