Table 1.
Kinetic parameters of functional turnover for the recovery of ME (3.2 μM, 1 min)‐induced inhibitory effect after β‐FNA (300 and 800 nM, 30 min) administration
β‐FNA 300 nM (n = 5) | β‐FNA 800 nM (n = 5) | |
---|---|---|
ME effect (%) | ||
Control | 99.5 ± 0.3 | 96.2 ± 1.4 |
t 30 = 0 min | 7.8 ± 2.6 | 7.8 ± 3.0 |
t 30 = 300 min | 69.8 ± 9.6 | 73.3 ± 9.6 |
Functional turnover of ME effect | ||
r′ (Emax · min−1) | 2.00 ± 0.13 | 1.78 ± 0.32 |
k′ (min−1) | 0.035 ± 0.007 | 0.024 ± 0.005 |
t ½′ (min) | 22 ± 3 | 36 ± 8 |
E ss (%) | 62.0 ± 7.9 | 77.0 ± 7.1 |
Functional turnover of μ receptor | ||
r (R t · min−1) | 0.25 ± 0.06* | 0.52 ± 0.20* |
k (min−1) | 0.022 ± 0.009 | 0.018 ± 0.004 |
t ½ (min) | 45 ± 9* | 44 ± 9 |
R ss (%) | 16 ± 3* | 37 ± 15* |
Values are expressed as mean ± SEM obtained by nonlinear regressions of n cells (see the Methods section). Parameters: r′ and k′ are the reappearance and disappearance rate constants of ME effect, t ½ ′ is the t 1/2 of ME effect, E ss is the maximal recovery of ME effect at steady state, r and k are the reappearance and disappearance rate constants of the receptor, t ½ is the t 1/2 of the receptor and R ss is the maximal recovery of the receptor at steady state.
P < 0.05, when compared with the corresponding parameter values for turnover of ME effect. No significant differences were found between the effects of the two concentrations of β‐FNA (300 and 800 nM).