RPR117824(RPR117824) - 药物靶点：AMPA receptor_在研适应症：脑缺血_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

AMPA receptor

作用机制

AMPA receptor拮抗剂(离子型谷氨酸受体AMPA拮抗剂)

治疗领域

神经系统疾病心血管疾病

在研适应症

脑缺血

非在研适应症-

原研机构

Aventis SA

在研机构

Aventis SA

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)-

特殊审评-

结构

分子式C16H11N3O5

InChIKeyKGABLDAFOWCUMF-UHFFFAOYSA-N

CAS号183734-76-1

关联

100 项与 RPR117824 相关的临床结果

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100 项与 RPR117824 相关的转化医学

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100 项与 RPR117824 相关的专利（医药）

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1

项与 RPR117824 相关的文献（医药）

2004-02-01·Mini-Reviews in Medicinal Chemistry3区 · 医学

Synthesis and Structure-Activity Relationships of 4,10-Dihydro-4-oxo-4HImidazo[ 1,2-a]Indeno[1,2-e]Pyrazine Derivatives: Highly Potent and Selective AMPA Receptor Antagonists with In Vivo Activity

3区 · 医学

Review

作者: Stutzmann, Jean-Marie ; Mignani, Serge ; Vuilhorgne, Marc

The excitatory neurotransmitter glutamate interacts with ionotropic and metabotropic receptors that mediate a variety of normal signalling processes in the brain. However, excessive stimulation of these receptors appears to be involved in neurodegenerative processes, at least in animal models. Ionotropic glutamate receptors can be divided into NMDA and non-NMDA (AMPA and KA) subtypes on the basis of t heir preferential affinities for the synthetic excitatory amino acids N-methyl-D-aspartic acid (NMDA) or 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl) propionic acid (AMPA), respectively. Although most of the early evidence favoured a role for NMDA receptors in the excitotoxic processes, it has been recognised that AMPA receptors may also be significantly involved in neuronal death. As a consequence, the synthesis of specific AMPA antagonists has raised much interest as source of potential drugs for epilepsy and acute and chronic neurodegenerative diseases. The discovery of RPR117824, a potent and selective AMPA receptors antagonist endowed with anticonvulsant and neuroprotective properties, induced growing interest on dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazine series. This review covers the main chemical course leading to the most promising compounds as well as the pharmacological properties of this original class of AMPA receptor antagonists.

100 项与 RPR117824 相关的药物交易

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