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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.