EAAT2 Activator Compounds for Glutamate Reuptake Enhancement
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Solution Overview
Problem
Existing treatments for neurological conditions associated with glutamate excitotoxicity, such as ischemic stroke, epilepsy, Alzheimer's disease, ALS, and depression, are inadequate in enhancing glutamate reuptake to prevent neuronal damage.
Innovation Solution
Development of compounds defined by Formula I, which increase the expression of excitatory amino acid transporter 2 (EAAT2) to enhance glutamate reuptake and reduce neuronal damage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for neurological conditions, then current therapeutic approaches are maintained, but glutamate reuptake enhancement is insufficient leading to neuronal damage
Solution Approach 1:
The patent applies parameter changes by modifying the expression level of EAAT2 transporter through compound administration. The compounds increase EAAT2 protein expression and function, changing the physiological parameter of glutamate reuptake capacity to prevent excitotoxicity and neuronal damage in neurological conditions
2Object-affected harmful factors
If EAAT2 expression is increased to enhance glutamate reuptake, then neuronal damage is reduced, but new compound development and administration are required
Solution Approach 1:
The patent uses small molecule compounds as intermediaries to activate EAAT2 expression. These compounds serve as mediators between the administered treatment and the desired physiological effect of increased glutamate reuptake, enabling neuronal protection without directly modifying the transporter gene
Data Source
Figure 1A~1B
Figure 2A~2C
Figure 3~4A
AI summary
Disclosed are compounds that activate excitatory amino acid transporter 2 (EAAT2), as well as methods of using these compounds to treat or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.