Modulator | log K_{B}^{a} | Log α^{b} | log(K_{B}/α)^{c} | ||
---|---|---|---|---|---|
Observed^{d} | Calculated^{e} | ||||
Gallamine | −6.03 ± 0.02 | −1.15 ± 0.08 (0.07) | −4.54 ± 0.15 | −4.88 ± 0.08 | |
Alcuronium | −5.92 ± 0.05 | 1.01 ± 0.10 (10.23) | −6.61 ± 0.08 | −6.93 ± 0.11 | |
C_{7}/3-phth | −6.75 ± 0.02 | −0.98 ± 0.01 (0.10) | −5.56 ± 0.11 | −5.75 ± 0.04 |
↵ a Logarithm of the equilibrium dissociation constant for the allosteric modulator at the free receptor, determined from a nonequilibrium binding assay using nonlinear regression according to eqs. 6 through 9 under Materials and Methods. Values represent the mean ± standard error of the mean of six experiments conducted in triplicate.
↵ b Logarithm of the cooperativity factor. Antilogarithm (geometric mean) is given in parentheses. All other details as in footnote a.
↵ c Logarithm of the equilibrium dissociation constant for the allosteric modulator at the [^{3}H]NMS-occupied receptor.
↵ d Determined from dissociation kinetic experiments using nonlinear regression according to eq. 5 under Materials and Methods. The value of the slope factor, n_{H}, was not significantly different from unity and was constrained as such, under which condition EC_{50} = K_{B}/α. Values represent the mean ± standard error of the mean of three experiments conducted in duplicate.
↵ e Calculated by dividing the dissociation constant of the modulator at the free receptor by the cooperativity factor determined for each individual nonequilibrium binding assay.