Table 2.
| Kinetic constants for σ1 receptor ligand binding. All data were obtained by scintillation proximity assay (SPA) at 23 °C. Errors represent standard deviation.
Constant | [3H](+)-pentazocine | [3H]haloperidol |
---|---|---|
Kd (nM): | 22.5 ± 10.8 | N.D. |
kslow (min−1)*: | (3.2 ± 0.6) × 10−3 | (4.4 ± 0.2) × 10−3 |
kfast (min−1) † | ||
at 1 nM: | (1.6 ± 0.6) × 10−2 | (2.8 ± 1.6) × 10−2 |
3 nM: | (2.3 ± 0.3) × 10−2 | (3.3 ± 0.2) × 10−2 |
10 nM: | (2.6 ± 0.4) × 10−2 | (4.3 ± 0.8) × 10−2 |
30 nM: | (3.0 ± 0.5) × 10−2 | N.D. |
100 nM: | (3.4 ± 0.4) × 10−2 | N.D. |
300 nM: | (3.4 ± 0.4) × 10−2 | N.D. |
koff (min−1) ‡ | ||
at 1 nM: | (9.4 ± 6.1) × 10−4 | (4.2 ± 1.6) × 10−4 |
3 nM: | (10.0 ± 7.0) × 10−4 | (5.1 ± 0.4) × 10−4 |
10 nM: | (8.0 ± 5.8) × 10−4 | (4.9 ± 0.6) × 10−4 |
30 nM: | (6.7 ± 4.8) × 10−4 | N.D. |
100 nM: | (5.1 ± 3.6) × 10−4 | N.D. |
300 nM: | (4.3 ± 2.9) × 10−4 | N.D. |
kslow is the observed rate constant for the slow step for ligand association to the σ1 receptor in the biphasic fit.
kfast is the observed rate constant for the fast step in ligand association to the σ1 receptor in the biphasic fit.
koff is the observed off rate for a given concentration in the SPA measurements, based on a monophasic fit.