|3-甲基-7-(四氢-2H-吡喃-4-基)-2-((反式-4-(三氟甲基)环己基)甲氧基)咪唑并[5,1-f][1,2,4]三嗪-4(3H)-酮|CsnPharm

CAS No.: 2007975-22-4

DSR-141562 Catalog No. CSN27184

Synonyms: LMN-75224

DSR-141562 is a novel orally available and brain-penetrant PDE 1 inhibitor. It has preferential selectivity for predominantly brain-expressed PDE1B over other PDE1 family members, and high selectivity for the PDE1 family over other PDE families and 65 other tested biologic targets.

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描述Cyclic nucleotide phosphodiesterases (PDEs) are enzymes that regulate intracellular signaling by catalyzing the hydrolysis of the second messenger 3',5'-cAMP and/or 3',5'-cGMP. DSR-141562 is a novel orally available and brain-penetrant PDE1 inhibitor with an IC₅₀ of 43.9 nM for human PDE1B. DSR-141562 (10 mg/kg; orally) slightly elevated the cGMP concentration, and it potently enhanced the increase of cGMP induced by a dopamine D₁ receptor agonist in mouse brains. The cGMP level in monkey cerebrospinal fluid was also elevated after treatment with DSR-141562 at 30 and 100 mg/kg and could be used as a translational biomarker. DSR-141562 (3-30 mg/kg) potently inhibited methamphetamine-induced locomotor hyperactivity in rats. Furthermore, DSR-141562 (0.3-3 mg/kg) reversed social interaction and novel object recognition deficits induced by repeated treatment with an N-methyl-D-aspartate receptor antagonist, phencyclidine, in mice and rats, respectively. In common marmosets, DSR-141562 (3 or 30 mg/kg) improved the performance in object retrieval with detour tasks. These results suggest that DSR-141562 is a therapeutic candidate for positive, negative, and cognitive symptoms in schizophrenia^[2].
参考文献

[1] Enomoto T, Tatara A, Goda M, 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. 2019;371(3):692-702. doi:10.1124/jpet.119.260869
[2] Enomoto T, 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. 2019 Dec;371(3):692-702

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4130 mL
- 12.0650 mL
- 24.1300 mL
- 5 mM
- 0.4826 mL
- 2.4130 mL
- 4.8260 mL
- 10 mM
- 0.2413 mL
- 1.2065 mL
- 2.4130 mL

技术信息

CAS号

2007975-22-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H25F3N4O3

运输

蓝冰

分子量

414.42

别名

LMN-75224

溶解度

DMSO	50.0 mg/mL (120.6 mM) warming

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