Table 2.
Influence of LUF6000 and LUF6096 on the rate of dissociation of [125I]I-AB-MECA binding from A3ARs
| k 1 (10−2 min−1) | k 2 (10−2 min−1) | Fraction of high affinity state | |
|---|---|---|---|
| Human | |||
| Vehicle | 1.21 ± 0.05 | 8.05 ± 2.22 | 0.56 ± 0.08 |
| LUF6000 (10 μM) | 0.49 ± 0.08* | 3.57 ± 1.09 (P = 0.11) | 0.56 ± 0.14 |
| LUF6096 (10 μM) | 0.75 ± 0.08* | 3.68 ± 1.13 (P = 0.10) | 0.65 ± 0.08 |
| Dog | |||
| Vehicle | 1.81 ± 0.22 | 40.1 ± 8.89 | 0.60 ± 0.04 |
| LUF6000 (10 μM) | 1.02 ± 0.02* | 21.3 ± 4.86 (P = 0.14) | 0.63 ± 0.05 |
| LUF6096 (10 μM) | 1.16 ± 0.06* | 28.9 ± 4.92 (P = 0.27) | 0.69 ± 0.05 |
| Rabbit | |||
| Vehicle | 0.60 ± 0.32 | 6.74 ± 1.50 | 0.74 ± 0.19 |
| LUF6000 (10 μM) | 0.62 ± 0.42 | 10.9 ± 2.39 | 0.52 ± 0.18 |
| LUF6096 (10 μM) | 0.60 ± 0.28 | 19.2 ± 6.93 | 0.82 ± 0.12 |
| Mouse | |||
| Vehicle | 1.00 ± 0.06 | 22.7 ± 3.04 | 0.69 ± 0.12 |
| LUF6000 (10 μM) | 0.95 ± 0.04 | 20.3 ± 9.74 | 0.64 ± 0.17 |
| LUF6096 (10 μM) | 0.93 ± 0.01 | 25.5 ± 11.0 | 0.62 ± 0.03 |
Data are dissociation rate constants (mean ± SEM; n = 3–6) calculated for the slow (K 1) and fast (K 2) components, as described in “Materials and methods”
*P < 0.05 vs. vehicle