Table 5.
Drug binding to plasma proteins in vitro and in vivo within the brain capillary.
| Drug | Plasma Protein | KDin vitro (μM) | KDin vivo (μM) | Reference |
|---|---|---|---|---|
| propranolol | bovine albumin | 299 ± 25 | 220 ± 40 | [1102] |
| AAG | 3.3 ± 0.1 | 19 ± 4 | ||
| bupivacaine | bovine albumin | 141 ± 10 | 211 ± 107 | [1113] |
| AAG | 6.5 ± 0.5 | 17 ± 4 | ||
| piroxicam | human albumin | 10.9 ± 0.1 | 910 ± 105 | [1114] |
| AAG | 29 ± 1 | 35 ± 3 | ||
| diazepam | bovine albumin | 2 | 13,900 | [1115] |
| human albumin | 6.3 ± 0.1 | 156 ± 35 | [1116] | |
| devazepide | human albumin | 8.2 ± 0.8 | 266 ± 38 | |
| imipramine | AAG | 4.9 ± 0.3 | 90 ± 9 | [1117] |
| isradipine | human albumin | 62 ± 8 | 221 ± 7 | [1118] |
| AAG | 6.9 ± 0.9 | 35 ± 2 | ||
| darodipine | human albumin | 94 ± 5 | 203 ± 14 | |
| AAG | 2.5 ± 0.5 | 55 ± 7 | ||
| domitroban | bovine albumin | 35 | 36 ± 4 | [1115] |
| L-tryptophan | bovine albumin | 130 ± 30 | 1700 ± 100 | [1119] |
| L-T3 | bovine albumin | 4.7 ± 0.1 | 46 ± 4 | [1100] |
| testosterone | bovine albumin | 53 ± 1 | 2520 ± 710 | [1100] |
AAG = human α1-acid glycoprotein; assumes 1 drug binding site on each plasma protein.