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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)
  1. Experiments performed in triplicate (n = 3).
  2. a)Tocris product information sheet.