Table 1.
Nicotine dose dependence (EC50) | Upregulation onset with nicotine addition |
Upregulation reversal with nicotine removal |
|||
---|---|---|---|---|---|
τ1 (h) | τ2 (h) | τ1 (h) | τ2 (h) | ||
α4β2 | a2.7×10−7 | 14.5a | 0.76 | 44 | |
Surface | ∼15a | 1.2 | 45 | ||
α6β2 | b4.6×10−5 | b1.2 | ND | 0.94 | ∼500 |
α3β2 | b1.3×10−4 | b1.5 | ND | ND | ND |
Cortical neurons | 9.2×10−8 | 1.1 | 12.5 | 0.45 | 295 |
Dose dependence of upregulation was measured by treating the HEK cells expressing nAChR subtypes or primary cultures of cortical neurons with increasing concentrations of nicotine and measuring increases in 125I-epi binding. Onset of upregulation was measured by treating cells with appropriate concentrations of nicotine as determined through dose dependence and measuring increases in 125I-epi binding as a function of time. Reversal of upregulation was initiated by treating the cells with appropriate concentrations of nicotine that cause maximum upregulation, washing the cells to remove nicotine, maintaining them in nicotine-free media, and measuring the 125I-epi binding as a function of time. ND, Not determined.
aTaken from Vallejo et al. (2005).
bTaken from Walsh et al. (2008).