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. 2017 Jul 7;174(16):2758–2772. doi: 10.1111/bph.13901

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).