TABLE 3

The blood and tissue concentrations and tissue-to-blood concentration ratios of small-molecule drugs in brain, spinal cord, sciatic nerve, and DRG at 6 hours in rats receiving constant intravenous infusion

DrugsaCbl (nM)Cbr (nM)Kp,brCsc (nM)Kp,scCsn (nM)Kp,snCdrg (nM)Kp,drg
Carbamazepine5455 ± 6256785 ± 9041.25 ± 0.219818 ± 9611.82 ± 0.319098 ± 15401.70 ± 0.4411,190 ± 11372.05 ± 0.06
Haloperidol134 ± 304423 ± 25934.5 ± 9.14400 ± 41534.0 ± 7.04235 ± 54833.5 ± 11.56560 ± 113352.5 ± 21.7
Ralfinamide694 ± 856665 ± 10219.79 ± 2.236260 ± 3989.09 ± 0.859305 ± 44013.6 ± 2.310,360 ± 240215.0 ± 3.1
Ranitidine1056 ± 186<30.0<0.02949.1 ± 8.40.047 ± 0.010749 ± 1490.710 ± 0.0761513 ± 731.46 ± 0.22
Atenolol2647 ± 9262.0 ± 12.20.023 ± 0.005171 ± 360.064 ± 0.0131855 ± 2250.701 ± 0.0873613 ± 2241.37 ± 0.12
Minoxidil1658 ± 541266 ± 190.170 ± 0.040439 ± 930.291 ± 0.1211473 ± 910.911 ± 0.2851573 ± 2790.987 ± 0.185
Dantrolene697 ± 26962.6 ± 11.70.077 ± 0.006118 ± 10.148 ± 0.026341 ± 1370.493 ± 0.081403 ± 1590.575 ± 0.093
Loperamide142 ± 4743.0 ± 9.50.327 ± 0.147154 ± 1151.16 ± 0.951022 ± 1577.63 ± 2.261278 ± 3129.20 ± 1.29
Mesoridazine391 ± 104224 ± 110.598 ± 0.126326 ± 300.873 ± 0.199954 ± 782.59 ± 0.801353 ± 1133.59 ± 0.69
Imatinib1785 ± 171112 ± 40.063 ± 0.006172 ± 300.096 ± 0.0091580 ± 1130.891 ± 0.0992475 ± 2871.39 ± 0.08
Cyclosporine A327 ± 53<6.46<0.020<4.80<0.01597.4 ± 24.00.299 ± 0.06662.8 ± 9.00.194 ± 0.033
  • a The dose for each drug is described in Materials and Methods. Four rats were used for each drug.