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| | DSR-141562 Basic information |
| Product Name: | DSR-141562 | | Synonyms: | DSR-141562;Imidazo[5,1-f][1,2,4]triazin-4(3H)-one, 3-methyl-7-(tetrahydro-2H-pyran-4-yl)-2-[[trans-4-(trifluoromethyl)cyclohexyl]methoxy]-;3-Methyl-7-(tetrahydro-2H-pyran-4-yl)-2-((trans-4-(trifluoromethyl)cyclohexyl)methoxy)imidazo[5,1-f][1,2,4]triazin-4(3H)-one;3-methyl-7-(oxan-4-yl)-2-{[(1r,4r)-4-(trifluoromethyl)cyclohexyl]methoxy}-3H,4H-imidazo[4,3-f][1,2,4]triazin-4-one | | CAS: | 2007975-22-4 | | MF: | C19H25F3N4O3 | | MW: | 414.42 | | EINECS: | | | Product Categories: | | | Mol File: | 2007975-22-4.mol |  |
| | DSR-141562 Chemical Properties |
| Boiling point | 516.1±60.0 °C(Predicted) | | density | 1.48±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | pka | -0.36±0.20(Predicted) | | form | Solid | | color | White to off-white |
| | DSR-141562 Usage And Synthesis |
| Uses | 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 IC50 of 43.9 nM, and the IC50 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[1][2]. | | 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[1].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[1].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[1].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[1]. | Animal Model: | Male SpragueDawley rats[1] | | 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[1] | | Dosage: | 0.3 mg/kg, 1 mg/kg or 3 mg/kg | | Administration: | Oral administration; single dose | | Result: | Reversed social interaction. |
| | IC 50 | PDE1 | | References | [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 DOI:10.1124/jpet.119.260869
[2] TakeshiEnomoto, 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 |
| | DSR-141562 Preparation Products And Raw materials |
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