TABLE 1

Dissociation rate constants (min−1) for [3H]NMS at human M2 mAChRs in CHO cells, determined in the absence or presence of 100 μM of the indicated allosteric modulatora


Modulator

Membranes

Intact Cells
None 0.84 ± 0.02 0.33 ± 0.06c
Gallamine 0.327 ± 0.024b 0.075 ± 0.012bc
Alcuronium 0.006 ± 0.001b 0.0006 ± 0.0006bc
C7/3-phth
0.036 ± 0.001b
0.008 ± 0.001bc
  • a Determined by nonlinear regression analysis according to eq. 4 under Materials and Methods. Parameter values represent the mean ± standard error of the mean of three experiments conducted in triplicate.

  • b Significantly (p < 0.05) different from the dissociation rate constant in the absence of modulator.

  • c Significantly (p < 0.05) different from the corresponding value obtained using CHO cell membranes.