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. 2008 Oct 24;283(43):29312–29321. doi: 10.1074/jbc.M803801200

FIGURE 5.

FIGURE 5.

The functional properties of McN-A-343 reflect a bitopic mode of orthosteric/allosteric interaction with the human M2 mAChR. A, interaction between ACh (left) or TMA (right) with McN-A-343 on M2 mAChR-mediated phosphorylation of ERK1/2 over 5 min at 37 °C in CHO-FlpIn cells stably expressing the M2 mAChR. Data represent the mean ± S.E. obtained from five experiments conducted in duplicate and are normalized to the maximum phospho-ERK1/2 response mediated by 3% FBS. Curves superimposed on the data points represent the best fit of an operational model of competitive (orthosteric) antagonism. B, ACh- or TMA-mediated ERK1/2 phosphorylation in the absence or presence of DDBL-4 for 5 min at 37 °C in CHO-FlpIn cells stably expressing the M2 mAChR. Data represent the mean ± S.E. obtained from six experiments conducted in duplicate. C, ACh-mediated [35S]GTPγS binding to activated G proteins in the absence or presence of DDBL-4 in CHO-FlpIn cell membranes stably expressing the wild type M2 mAChR. Data represent the mean ± S.E. obtained from three experiments conducted in duplicate.