Table 2. hM4 Potency, M2 Selectivity, CYP Inhibition, and P-gp Efflux for Compounds 11a and 11b.

Calcium mobilization assays with (a) hM4. IC50 values for hM4 represent means from at least three (n = 3) independent experiments performed in triplicate.
hM2/Gqi5-CHO cells performed in the presence of an EC80 fixed concentration of acetylcholine. IC50 values for hM2 represent one independent experiment performed in triplicate.
Cytochrome P450 cocktail inhibition assay in human liver microsomes (see SI for further details).
BBB penetration potential using MDR1-MDCK cell monolayers; ER is defined as Papp(B-to-A)/Papp(A-to-B) (see SI for further details).
Calculated using ChemDraw Professional version 20.1.
