DSR-141562

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC 50 of 43.9 nM, and the IC 50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia In Vivo DSR-141562 (oral administration; 30 mg/kg; single dose; plasma and brain exposures 0.5, 1, 2, and 3 hours after administration) exhibits good brain uptake, with the brain-to-blood concentration ratio of unbound drug being 0.99 in rats. DSR-141562 (oral administration; 10 mg/kg; single dose; 2 hours) slightly but significantly increases cGMP contents in the frontal cortex and striatum in rat . DSR-141562 (oral administration; 30 mg/kg or 100 mg/kg; single dose; 2 hours) causes a significant increase in cGMP concentration in monkey CSF. The plasma concentrations of unbound this compound are above 43.9 nM (IC50s)for PDE1B in vitro (43.9 nM). DSR-141562 causes a significant increase in cGMP concentration in monkey CSF . DSR-141562 (oral administration; 3 mg/kg, 10 mg/kg and 30 mg/kg; single dose) significantly reverses methamphetamine-induced locomotor hyperactivity, but has no effect on spontaneouslocomotor activity at 3 and 10 mg/kg . DSR-141562 (oral administration; 0.3 mg/kg, 1 mg/kg or 3 mg/kg) significantly reversed the phencyclidine-induced decrease of social interaction time in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SpragueDawley rats Dosage: 3 mg/kg, 10 mg/kg and 30 mg/kg Administration: Oral administration; single dose Result: Inhibited methamphetamine-induced locomotor hyperactivity in rats, while it had only minimal effects on the spontaneous locomotor activity. Animal Model: Male SpragueDawley rats Dosage: 0.3 mg/kg, 1 mg/kg or 3 mg/kg Administration: Oral administration; single dose Result: Reversed social interaction. IC50& Target:IC50: 43.9 nM (human PDE1B) IC50: 97.6 nM (human PDE1A) IC50: 431.8 nM (human PDE1C)

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