Table 1 Overview of positron emission studies used for modeling the dose-blockade relationship of intravenous naloxone and oral naltrexone.
Antagonist | Method | N | Measurement time point | Dose | MOR blockade |
|---|---|---|---|---|---|
Intravenous naloxone | |||||
Frost et al. (1985) [12] | PET | 1 | 35–65 min | 1 mg/kg | 83% |
90% | |||||
Mayberg and Frost (1990) [13] | PET | --- | 45–65a min | 0.001 mg/kg | 19% |
0.01 mg/kg | 65% | ||||
0.1 mg/kg | 97% | ||||
1.0 mg/kg | 98% | ||||
Kim et al. (1997) [24] | Dual-detector | 8 | 45–65 min | 0.002 mg/kg | 43% |
0.03 mg/kg | 81% | ||||
Villemagne et al. (1994) [28] | Dual-detector | 24 | 45–65 min | 0 mg/kg | 0% |
0.0005 mg/kg | 20% | ||||
0.001 mg/kg | 40% | ||||
0.005 mg/kga | 75% | ||||
0.01 mg/kg | 100% | ||||
0.1 mg/kg | 100% | ||||
0.5 mg/kga | 100% | ||||
1.0 mg/kg | 100% | ||||
Oral naltrexone | |||||
Rabiner et al. (2011) [23] | PET | 20 | < 8 h | 2 mg | 27% |
5 mg | 43% | ||||
5 mg | 46% | ||||
5 mg | 58% | ||||
15 mg | 61% | ||||
50 mg | 92% | ||||
50 mg | 98% | ||||
