Glutamate Receptor Antagonist Development for Stroke

During cerebral ischemia, glutamate is released in supraphysiological amounts that are toxic to brain tissue. This excitotoxicity is mediated by several glutamate receptor subtypes, including the ionotropic N-methyl-D-aspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propanoic acid (AMPA) receptors. Multiple downstream death signaling cascades can be terminated at upstream initiation points to control the increase in extracellular glutamate, thereby providing neuroprotection. Because of the role of glutamate in the excitotoxicity cascade, glutamate receptors are likely candidates for the development of neuroprotective drugs, providing a source of novel strategies for investigating new protective therapies for stroke.

Fig. 1. The balance of ion and glutamate concentration at neuro synapses. (Shen et al., 2022)

Our Glutamate Receptor Antagonist Development Services

Ace Therapeutics is a leading preclinical CRO in the field of stroke research, dedicated to developing strategies against glutamate-mediated excitotoxicity. Our drug discovery team provides reliable preclinical glutamate antagonist development services from target identification to preclinical testing to clients worldwide.

Our team consists of experts from diverse backgrounds, including neuroscience, medicinal chemistry, pharmacology, and bioinformatics, and actively collaborates with academic institutions and biopharmaceutical companies to advance your stroke drug development program.

What Glutamate Antagonists Can We Develop?

• NMDA Receptor Antagonists
• AMPA Receptor Antagonists
• Metabotropic Glutamate Receptors (mGluRs) Antagonists

Glutamate Antagonist Development Process

Discovery and Optimization of Glutamate Antagonists

We use a variety of techniques, including high-throughput screening, molecular modeling, medicinal chemistry, structural biology, and computational chemistry, to rapidly identify lead compounds with the potential to modulate glutamate receptor activity. In addition, we screen compounds to discover compounds that interact with these targets. Through iterative cycles of design, synthesis, and testing, we optimize these lead compounds to improve their potency, selectivity, and pharmacokinetic properties to ensure they are suitable for further development.

Preclinical Studies for Glutamate Antagonists

We provide rigorous preclinical testing of glutamate antagonists to evaluate their safety and efficacy in animal and in vitro models of stroke. Through careful experimental design and data analysis, we can assess the ability of glutamate antagonists to reduce neuronal damage, improve functional outcomes, and minimize adverse effects.

• Monitoring of physiological parameters during stroke
• Neurobehavioral assessment
• Histological analysis
• Infarct volume measurement
• BBB permeability assessment

At Ace Therapeutics, we pride ourselves on our commitment to excellence and innovation in stroke drug development. We are your trusted partner in providing comprehensive services for the development of glutamate receptor antagonists. If you are interested in our services, please do not hesitate to contact us!

1. Shen, Z., et al. (2022). Glutamate excitotoxicity: Potential therapeutic target for ischemic stroke. Biomedicine & Pharmacotherapy, 151, 113125.