PDM-042

PDM-042 is a potent, selective, orally active, and brain-penetrable small molecule inhibitor of **phosphodiesterase 10A (PDE10A)**. It demonstrates high selectivity for PDE10A over other phosphodiesterases, with IC50 values less than 1 nM and over 1000-fold selectivity. Preclinical studies have shown that PDM-042 has good oral bioavailability (~33%), excellent brain penetration, and high target occupancy in rat brain. It modulates corticostriatal neurotransmission, affects medium spiny neuron activity, and demonstrates dose-dependent effects on L-DOPA-induced abnormal involuntary movements (AIMs) in animal models. PDM-042 has been investigated primarily for its antipsychotic-like and antidyskinetic effects, with potential applications in the treatment of **schizophrenia** and **Parkinson’s disease-related dyskinesia**. Cognitive enhancing effects and minimal cataleptic liability have also been observed in animal models. The structure is a triazolopyrazine-containing pyrimidinylmorpholine derivative[3][5][7][1].

Other names

(E)-4-(2-(2-(2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)vinyl)-6-(pyrrolidin-1-yl)pyrimidin-4-yl)morpholine)