PCS1055 inhibits G protein activation in a concentration-dependent manner, with the highest potency at the M4 receptors. Both studies show that PCS1055 is most potent at the M4 receptor subtype with a binding preference of 130-, 31.2-, 426- and >1000-fold, and functional preference of 255-, 69.1-, 342- and >1000-fold over the M1-, M2-, M3- and M5 receptors, respectively. PCS1055 also antagonized functional signal transduction as demonstrates by the inhibition of agonist-stimulated GTP-γ-[35S] binding [1].

PCS1055 (30 mg/kg; intraperitoneal injection; male mice) treatment displays the maximal plasma levels at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. At 1 h, the maximal compound exposure observed in the brain is 11.8 nM [1].