Pharmacological characterization of [3H]PK11195 and [3H]Ro5-4864 binding to Jurkat cell line membranes
Jurkat cells membranes were incubated with 1.5 μM [3H]PK11195 or [3H]Ro5-4864 and increasing drug concentrations. The IC50 values were calculated, and the Ki inhibitory constant was derived (Cheng and Prusoff, 1973). Each value represents the mean ± S.E.M. of three experiments, each performed in triplicate.
| Compound | Ki or Percentage of Inhibition | |
|---|---|---|
| vs [3H]PK11195 | vs [3H]Ro5-4864 | |
| μM | ||
| PK11195 | 1.90 ± 0.20 | 3.68 ± 0.35 |
| Ro5-4864 | 32.3 ± 4.00 | 8.74 ± 0.79 |
| Diazepam | 79.0 ± 8.00 | 18.4 ± 1.90 |
| Clonazepam | No displacement up to 10-4 M | 35 ± 4% at 10-4 M |