Table 1.
Displacer of [3H]-DPA-713 | Dissociation Parameters | ||||||||
---|---|---|---|---|---|---|---|---|---|
C/C | C/T | T/T | |||||||
koff | RT | t1/2 | koff | RT | t1/2 | koff | RT | t1/2 | |
DPA-713 (12 μM) | 0.74 | 1.35 | 0.94 | 0.76 | 1.28 | 0.92 | 0.56a | 1.78 | 1.24 |
DPA-713 (12 μM) + PK11195 (5 μM) | 0.76 | 1.31 | 0.91 | 0.75 | 1.33 | 0.93 | 1.90a | 0.52 | 0.36 |
DPA-713 (12 μM) + Cholesterol (1.2 μM) | 0.65 | 1.53 | 1.07 | 0.72 | 1.38 | 0.96 | 1.58a | 0.63 | 0.43 |
One phase exponential decay fits for T/T dissociation traces (Fig 1f) exhibit 95% confidence interval that koff for [3H]-DPA-713 is faster when PK 11195 or cholesterol are present than when [3H]-DPA-713 dissociates in the presence of DPA-713.