B[a]P-7,8-dione modulates the binding kinetics of [3H]ryanodine to RyR1 in a concentration-dependent manner.
| Control | B[a]P-7,8-dione, 0.1 μM | B[a]P-7,8-dione, 1 μM | |
|---|---|---|---|
| k obs(min−1) | 0.0314 ± 0.0014 | 0.0642 ± 0.0134 | 0.193 ± 0.018 |
| T1/2 (min) | 22.1 ± 0.9 | 11.1 ± 2.2 | 3.6 ± 0.3 |
| Beq (pmol/mg)1-aa | 2.81 ± 0.24 | 2.20 ± 0.28 | 1.48 ± 0.04 |
↵1-a a [3H]Ryanodine occupancy at steady state
k obs, observed association rate constant; T1/2, half-time to steady state.