TABLE 2

The percent unbound fractions of small-molecule drugs in blood, brain, spinal cord, sciatic nerve, and DRG

Drugsfu,bl (%)afu,br (%)afu,sc (%)afu,sn (%)afu,drg (%)a
Carbamazepine26.6 ± 1.713.5 ± 0.613.8 ± 0.610.2 ± 1.015.8 ± 1.9
Haloperidolb9.71 ± 1.261.32 ± 0.220.89 ± 0.330.68 ± 0.091.19 ± 0.28
Ralfinamide13.8 ± 0.32.36 ± 0.171.32 ± 0.072.25 ± 0.304.59 ± 0.57
Ranitidine47.3 ± 4.185.3 ± 52.562.7 ± 20.920.5 ± 6.246.8 ± 7.6
Atenolol41.5 ± 1.359.9 ± 6.771.3 ± 12.239.6 ± 9.342.9 ± 13.5
Minoxidil64.0 ± 7.065.8 ± 30.050.1 ± 5.956.7 ± 13.4100 ± 0c
Dantrolene3.08 ± 0.584.63 ± 0.883.32 ± 0.312.39 ± 0.887.74 ± 2.79
Loperamide2.99 ± 0.080.58 ± 0.010.44 ± 0.060.22 ± 0.020.46 ± 0.10
Mesoridazine9.66 ± 0.741.70 ± 0.021.62 ± 0.320.86 ± 0.081.66 ± 0.33
Imatinib4.20 ± 0.512.15 ± 0.141.84 ± 0.501.18 ± 0.102.17 ± 0.24
Cyclosporine A0.042 ± 0.0100.011 ± 0.0000.018 ± 0.0100.031 ± 0.0360.033 ± 0.007
GF1209180.015 ± 0.0020.011 ± 0.0020.0069 ± 0.00040.0064 ± 0.00100.0037 ± 0.0002
Amantadine89.9 ± 10.416.0 ± 1.88.47 ± 1.2510.6 ± 0.918.5 ± 3.3
Amitriptyline5.90 ± 0.560.38 ± 0.070.28 ± 0.030.30 ± 0.020.51 ± 0.04
Citalopram18.5 ± 1.62.06 ± 0.091.23 ± 0.221.98 ± 0.113.57 ± 0.37
Clozapine6.04 ± 0.250.94 ± 0.150.46 ± 0.060.55 ± 0.040.97 ± 0.22
Fluphenazine0.75 ± 0.100.069 ± 0.0060.037 ± 0.0030.036 ± 0.0020.060 ± 0.006
Granisetron42.3 ± 6.112.1 ± 1.99.85 ± 1.2012.3 ± 1.417.1 ± 1.6
Loxapine3.10 ± 0.260.36 ± 0.040.28 ± 0.020.19 ± 0.010.48 ± 0.02
Maprotiline4.08 ± 0.310.23 ± 0.090.14 ± 0.020.14 ± 0.010.27 ± 0.02
Nortriptyline4.12 ± 0.280.27 ± 0.040.15 ± 0.010.19 ± 0.010.35 ± 0.01
Risperidone11.8 ± 2.97.61 ± 0.405.78 ± 0.426.97 ± 0.6910.9 ± 2.2
  • a Data were presented as mean ± S.D. from three independent measurements unless otherwise indicated.

  • b Data were presented as mean ± S.D. from six independent measurements.

  • c Concentrations in the receiver compartment were similar to or exceeded slightly those in the donor compartment. Thus, the unbound fraction in DRG was taken as 100%.