Table 2. Equilibrium Constants Measured for Various Drugs with Soluble HSA by Using Ultrafast Affinity Extraction on HSA Microcolumnsa.
association equilibrium constant, Ka, or global affinity
constant, nKa′ (M–1) | |||
---|---|---|---|
drug | estimate (eq 6) | estimate (eqs 5 and 6) | literature [ref] |
warfarin | 2.4 (±0.4) × 105 | 1.6 (±0.2) × 105 | 2.0–5.7 × 105 [18, 29, 30] |
tolbutamide | 1.1 (±0.4) × 105 | 0.9 (±0.2) × 105 | 1.1 (±0.1) × 105 [19]b |
acetohexamide | 1.8 (±0.5) × 105 | 1.3 (±0.1) × 105 | 1.7(±0.1) × 105 [20]b |
verapamil | 1.5 (±0.4) × 104 | 1.6 (±0.2) × 104 | 1.4 (±0.1) × 104 [21]c |
gliclazide | 8.0 (±0.6) × 104 | 6.9 (±1.0) × 104 | 7.9 (±0.1) × 104 [22]b |
chlorpromazine | 6.2 (±0.5) × 104 | 4.9 (±0.5) × 104 | 6.4 × 104 [23] |
These results were measured at pH 7.4 and at 37 °C. The values in parentheses represent a range of ±1 S.D., as determined by error propagation.
The global affinity constants for these drugs were calculated from data in the given references.
This value represents the average association equilibrium constant for R- and S-verapamil at their high affinity site on HSA.