CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A ( PDE10A ) inhibitor with IC 50 values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC 50 of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia.
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