AMG-579

AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Neurological Disease

IC50: 0.1 nM (Phosphodiesterase 10A)[1]

AMG 579 shows statistically significant reduction of PCP induced behavior in rats over the 2 h period. Minimum effective doses for efficacy in PCP-LMA model is determined to be 0.3 mg/kg for AMG 579. In dog, 5 exhibits superior oral bioavailability of 72%[1].

Rats[1] Adult male Sprague−Dawley rats (250−280 g) are dosed at 0.1, 0.3, 1, and 3 mg/kg PO 1 h prior to administration of PCP. The magnitude of rat locomotor activity is quantified as number of beam breaks over a 2 h period[1].

[1]. Hu E,et al. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41.

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