Table 2. Binding affinity at human opioid receptors.
Ki (nM) | |||||
---|---|---|---|---|---|
Drug | μ | δ | κ | ORL1 | Reference |
Buprenorphine | 0.0027 | 33 | 0.0021 | 25,000 | [60] |
Steady state free Cmax = 0.87 nM | 0.52 | [61] | |||
0.08 | 0.42 | 0.11 | 285 | [37] | |
1.5 | 6.1 | 2.5 | 77.4 | [62] | |
1.5 | 4.5 | 0.8 | [63] | ||
0.21 | [64] | ||||
0.21 | 2.9 | 0.62 | [65] | ||
1.8 | [66] | ||||
1.5 | 4.5 | 0.8 | [67] | ||
Norbuprenorphine | 0.0018 | 1300 | 0.0013 | [60] | |
Steady state total Cmax = 22 nM | 0.07 | 3.17 | 0.91 | 7330 | [37] |
Methadone | 14 | [61] | |||
Free Cmax = 438 nM | 3.7 | [68] | |||
5.6 | [69] | ||||
0.6 | 132.2 | 323.5 | [63] | ||
3.37 | [37] | ||||
7.7 | [66] | ||||
3.38 | [64] | ||||
Naltrexone | 1.1 | [61] | |||
Free Cmax = 28 nM | 0.26 | 117 | 5.15 | [70] | |
0.2 | 10.8 | 4 | [63] | ||
0.5 | 1 | [71] | |||
Naloxone | 3.3 | [61] | |||
Free Cmax = 13 nM | 0.8 | [68] | |||
0.79 | 76 | 1.1 | [72] | ||
2.4 | [73] | ||||
1.4 | 67.5 | 2.5 | [63] | ||
3 | [74] | ||||
1.51 | [64] | ||||
7 | 4 | [71] | |||
0.66 | 120 | 1.2 | [65] | ||
0.6 | [66] |