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Table 2 Pharmacokinetic parameters of nor-BNI, GNTI and JDTic (·2HCl salts, 10 mg kg-1i.p.), estimated using non-compartmental analysis

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
  1. a) From postmortem samples, 13–18 minutes after 39 mg kg-1 GNTI·2CF3CO2H.
  2. Abbrevations: AUC, area under curve; CL, clearance; Cmax, maximal mean concentration; F, bioavailability; p, plasma; tmax, time at Cmax; u, unbound (free); Vz, terminal-phase apparent volume of distribution.