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. 2020 Nov 6;15(11):e0241362. doi: 10.1371/journal.pone.0241362

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]