Usage recommendations for probe JNJ-42396302 and control JNJ-40573663
In cells
Use at concentration up to 10 µM.
We recommend to use the PDE10A inhibitor THPP-1 also available from SGC for control experiments.
Use the recommended concentration to avoid off-target toxicity and/or off-target activity. Using concentrations that are higher than recommended could lead to false positive or confounding results.
In vivo
Tested in various animals: Dose-and time-dependent occupancy of rat brain PDE10 shown: Maximum occupancy was observed 1 hour after p.o. dosing (ED50: 1.4 mg/kg). The time-course experiment showed a gradual decrease of PDE10 occupancy over time, with 50% occupancy up to 8 h after dosing (10 mg/kg, p.o.).