FCPE07(FCPE07) - 药物靶点：PDE4D_在研适应症：抑郁症_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

PDE4D

作用机制

PDE4D抑制剂(phosphodiesterase 4D inhibitors)

治疗领域

其他疾病

在研适应症

抑郁症

非在研适应症-

原研机构

南方医科大学

在研机构

南方医科大学

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

结构

分子式C21H23F2NO4

InChIKeyDBNDIIUELFNMBG-UHFFFAOYSA-N

CAS号2033167-05-2

关联

100 项与 FCPE07 相关的临床结果

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100 项与 FCPE07 相关的转化医学

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100 项与 FCPE07 相关的专利（医药）

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1

项与 FCPE07 相关的文献（医药）

2017-01-18·ACS Chemical Neuroscience3区 · 医学

Discovery of N-Alkyl Catecholamides as Selective Phosphodiesterase-4 Inhibitors with Anti-neuroinflammation Potential Exhibiting Antidepressant-like Effects at Non-emetic Doses

3区 · 医学

Article

作者: Wang, Hai-Tao ; Yang, Xue-Mei ; Zhou, Zhong-Zhen ; Xu, Jiang-Ping ; Cheng, Yu-Fang ; Yu, Hui ; Ge, Bing-Chen ; Huang, Cang ; Zou, Zheng-Qiang

Depression involving neuroinflammation is one of the most common disabling and life-threatening psychiatric disorders. Phosphodiesterase 4 (PDE4) inhibitors produce potent antidepressant-like and cognition-enhancing effects. However, their clinical utility is limited by their major side effect of emesis. To obtain more selective PDE4 inhibitors with antidepressant and anti-neuroinflammation potential and less emesis, we designed and synthesized a series of N-alkyl catecholamides by modifying the 4-methoxybenzyl group of our hit compound, FCPE07, with an alkyl side chain. Among these compounds, 10 compounds displayed submicromolar IC₅₀ values in the mid- to low-nanomolar range. Moreover, 4-difluoromethoxybenzamides 10g and 10j, bearing isopropyl groups, exhibited the highest PDE4 inhibitory activities, with IC₅₀ values in the low-nanomolar range and with higher selectivities for PDE4 (approximately 5000-fold and 2100-fold over other PDEs, respectively). Furthermore, compound 10j displayed anti-neuroinflammation potential, promising antidepressant-like effects, and a zero incidence rate of emesis at 0.8 mg/kg within 180 min.

100 项与 FCPE07 相关的药物交易

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