Table 1 Physicochemical properties and plasma and brain homogenate binding of nor-BNI, GNTI, JDTic, and naltrexone
From: Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
Nor-BNI | GNTI | JDTic | Naltrexone | |
|---|---|---|---|---|
Salt tested | 2HCl·H2O | 2HCl·1.5H2O | 2HCl·H2O | HCl·2H2O |
Water solubility (mmol L-1, 25 °C) | >45 | >100a | >45 | >100a |
mean | ||||
(95% CI) | ||||
Log10D7.4 | 1.5 | -0.1 | 1.8 | 0.86 |
octanol:buffer (pH 7.4) | (1.3; 1.8) | (-0.2; 0) | (1.7; 2.0) | (0.82; 0.90) |
Fraction unbound (%) | ||||
Plasma | 51 | 28 | 19 | 83 |
(44; 59) | (24; 31) | (17; 21) | (72; 94) | |
Brain homogenate | 12 | 7 | 7 | 47 |
(10; 17) | (6; 9) | (6; 8) | (34; 65) |