CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.
CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.
CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.
CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.
Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.
Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.
