TABLE 1

Operational model parameters for the interaction between CCh and brucine at the rM3Δi3K7.32E mAChR in yeast

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

Gpa1/GαqGpa1/Gα12
Log KB−4.48 ± 0.13 −4.89 ± 0.13
Log τB0.15 ± 0.07 (τB = 1.4)−0.79 ± 0.17** (τB = 0.16)
Log αβ0.76 ± 0.17 (αβ = 5.8)1.06 ± 0.10 (αβ = 11.5)

  • 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 Student's t test (compared with the same parameter in the Gpa1/Gαq strain).