TABLE 4

Operational model parameters for the interaction between CCh and brucine at the M3K7.32E mAChR

Data are presented as the mean ± S.E.M. of three to six separate experiments performed in duplicate.

Ca2+ MobilizationMembrane RufflingERK1/2 PhosphorylationERK1/2 Phosphorylation + PTX
Log KB−5.17 ± 0.15−4.61 ± 0.13−5.21 ± 0.28−5.30 ± 0.19
Log τB0.41 ± 0.03**B = 2.6)−1.40 ± 0.48 (τB = 0.04)−0.66 ± 0.16 (τB = 0.2)−0.43 ± 0.16 (τB = 0.4)
Log αβ0.70 ± 0.17 (αβ = 5.0)0.88 ± 0.10 (αβ = 7.6)0.84 ± 0.06 (αβ = 6.9)0.84 ± 0.07 (αβ = 6.9)
  • Log KB, logarithm of the dissociation constant of the allosteric modulator; Log τB, logarithm of the operational efficacy of the allosteric modulator; Log αβ, logarithm of the cooperativity of the allosteric modulator on the potency of the orthosteric agonist.

  • ** P < 0.01 determined by one-way ANOVA with Newman-Keuls multiple comparisons post test across Log τB values (statistically different to the Log τB value derived for membrane ruffling).