TABLE 4

Operational model pKB and Schild slope estimates for McN-A-343, AC-42, and 77-LH-28-1 at the M2-WT and M2-EDGE-YT mAChRs from interaction studies with ACh in assays of ERK1/2 phosphorylation

Values represent the mean ± S.E.M. obtained from four to five experiments conducted in duplicate. pKB is the negative logarithm of the equilibrium dissociation constant, determined with the Schild slope constrained to equal 1

M2-WT M2-EDGE-YT
pKB Schild Slope pKB Schild Slope
McN-A-343 4.69 ± 0.10 1.19 ± 0.12 N.P. N.P.
AC-42 5.86 ± 0.11 0.92 ± 0.13 6.10 ± 0.13 1.15 ± 0.14
77-LH-28-1 5.95 ± 0.15 1.00 ± 0.16 6.44 ± 0.11* 0.97 ± 0.13
  • N.P., not performed.

  • * Significantly different (P < 0.05) from the corresponding control value at the same receptor.