Concentrations of naltrexone and 6β-naltrexol in plasma and brain tissue after i.p. injection in mice
The two compounds were extracted from plasma or brain tissue homogenates and measured by liquid chromatography/tandem mass spectrometry, using atmospheric pressure chemical ionization/positive ionization. Nalbuphine served as the internal standard. The method was sensitive to ∼1 ng/ml (g) (3-4 nM). 6β-Naltrexol was detectable in plasma but not brain tissue after the naltrexone dose (1.9 ng/ml and 1.7 ng/ml after 10 and 60 min, respectively). In contrast, no naltrexone was detectable after administration of 6β-naltrexol. The concentrations of two compounds in each row of the table represent the injected parent drug only. Data are mean ± S.D., n = 3.
Injection | Plasma Concentration at Time after Injection (min) | Brain Concentration at Time after Injection (min) | ||||
---|---|---|---|---|---|---|
10 | 60 | 10 | 60 | |||
ng/ml | ng/g | |||||
Naltrexone, 1 mg/kg | 54 ± 16 | 4 ± 1 | 69 ± 20 | 9 ± 1 | ||
6β-Naltrexol, 1 mg/kg | 61 ± 7 | 24 ± 28 | 7 ± 6 | 9 ± 1 | ||
6β-Naltrexol, 10 mg/kg | 857 ± 122 | 75 ± 25 | 89 ± 6 | 74 ± 14 |