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Antagonist properties at M2 mutant receptors.
| GABA pEC50 (EC50) | α-endosulfan pIC50 (IC50) | Proadifen pIC50 (IC50) | |
|---|---|---|---|
| Wild Type | 2.78 ± 0.04 (1.6 mM) | 4.77 ± 0.15 (17 μM) | 5.09 ± 0.04 (8.1 μM) |
| Q2′N | 2.74 ± 0.02 (1.8 mM) | NI (>100 μM) | 5.54 ± 0.09 (2.9 μM) |
| T6'S | 2.75 ± 0.02 (1.8 mM) | NI (>100 μM) | 5.29 ± 0.04 (5.1 μM) |
NI = IC50 was not reached at the highest concentration tested (10−4 M). See Fig. 4D.
