TABLE 2

Agonist coupling efficiency parameters for M1 mAChR-mediated Ca2+ elevation in U2OS cells

Data represent the mean ± S.E.M. of four to eight experiments performed in duplicate. The logarithm of the relative coupling efficiency parameter, τ, was determined via nonlinear regression of the data to an operational model of agonism and corrected for receptor expression levels to yield a corrected τc parameter (Logτc). Antilogarithm shown in parentheses.

LigandLogτc
Wild Type (0.5 pfu/ml)F77I (1.25 pfu/ml)W101A (0.5 pfu/ml)Y381A (0.5 pfu/ml)
Acetylcholine2.82 ± 0.072.83 ± 0.082.83 ± 0.072.23 ± 0.07*
(661)(676)(676)(169)
Pilocarpine0.70 ± 0.060.44 ± 0.060.91 ± 0.07−2.73 ± 0.94*
(5)(2.8)(8.1)(0.002)
AC-420.01 ± 0.05−1.85 ± 0.58*1.26 ± 0.06*−0.77 ± 0.09
(1)(0.014)(18.2)(0.17)
77-LH-28-10.62 ± 0.06−0.69 ± 0.11*0.33 ± 0.06−0.85 ± 0.10*
(4.2)(0.20)(2.13)(0.14)
  • * Significantly different (p < 0.05) from the wild-type receptor as determined by one- way ANOVA followed by Dunnett's post test.