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DSR-141562

Catalog No. T39421 CAS 2007975-22-4

DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.

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DSR-141562, CAS 2007975-22-4

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Description	DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.
Targets&IC50	PDE1B (human):43.9 nM (IC50), PDE1A (human):97.6 nM (IC50), PDE1C (human):431.8 nM (IC50)
In vivo	DSR-141562, when administered orally to rats and monkeys, demonstrates effective brain uptake and pharmacological activity across multiple dosages and time points. At a single dose of 30 mg/kg, it achieves good brain penetration, evidenced by a brain-to-blood concentration ratio of 0.99 in rats, and exhibits significant pharmacological effects at various intervals post-administration (0.5, 1, 2, and 3 hours). A lower dose of 10 mg/kg, given 2 hours prior, modestly yet significantly enhances cGMP levels in the frontal cortex and striatum of rats. This compound, at doses of 30 mg/kg or 100 mg/kg, notably increases cGMP concentration in monkey cerebrospinal fluid (CSF) after 2 hours, with plasma concentrations of the unbound drug exceeding 43.9 nM, which is its IC50 for PDE1B inhibition in vitro. Furthermore, DSR-141562 effectively counteracts methamphetamine-induced hyperactivity in rats at 3 mg/kg, 10 mg/kg, and 30 mg/kg doses without affecting spontaneous locomotor activity at the lower doses of 3 and 10 mg/kg. Likewise, it significantly mitigates the phencyclidine-induced decline in social interaction in mice at doses of 0.3 mg/kg, 1 mg/kg, and 3 mg/kg. These findings demonstrate DSR-141562's potential in modulating neural activity and behavior in animal models through its pharmacological actions on cGMP levels and its ability to penetrate the brain, suggesting its therapeutic relevance.

Molecular Weight	414.42
Formula	C19H25F3N4O3
CAS No.	2007975-22-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Takeshi Enomoto, et al.A Novel Phosphodiesterase 1 Inhibitor DSR-141562 Exhibits Efficacies in Animal Models for Positive, Negative, and Cognitive Symptoms Associated With Schizophrenia. J Pharmacol Exp Ther 2. Takeshi Enomoto, et al. The Preclinical Profile of DSR-141562: A Novel Phosphodiesterase 1 Inhibitor for the Treatment of Positive Symptoms, Negative Symptoms and Cognitive Impairments Associated with Schizophrenia.Proceedings for The 93rd Annual Meeting of the Japanese Pharmacological Society

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Keywords

DSR-141562 2007975-22-4 DSR 141562 DSR141562 inhibitor inhibit

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