AMPA Receptor Antagonist Development for Stroke

Excitotoxicity in ischemic stroke is mediated by several glutamate receptor subtypes, including the ionotropic N-methyl-D-aspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors. Clinical trials of drugs that block NMDA receptors for the treatment of acute ischemic stroke have been disappointing. The AMPA receptor differs from the NMDA receptor in several important ways. It is the primary mediator of fast excitatory neurotransmission. This ligand-gated cation channel is primarily permeable to sodium rather than calcium. It is found in both gray and white matter. The AMPAR antagonists have been shown to be neuroprotective in stroke models and represent a fruitful approach for the development of neuroprotective drugs.

Fig. 1. Suggested mechanism of AMPA receptor antagonist perampanel-mediated neuroprotection in the treatment of cerebral ischemia. (Suda et al., 2019)

Our AMPAR Antagonist Development Services

Ace Therapeutics is a leading global provider of stroke drug development services. We are proud to offer AMPAR antagonist development services to pharmaceutical companies. Our team of scientists and researchers have in-depth knowledge of the role of AMPAR in stroke. We work closely with pharmaceutical companies, academic institutions, and research organizations to understand their specific needs and goals.

Our laboratories are equipped with advanced molecular biology, cell culture, electrophysiology, and high-throughput screening tools, enabling us to conduct cutting-edge research in AMPAR antagonist development. We offer a full range of preclinical services spanning the drug development process from AMPAR target identification to preclinical efficacy evaluation. We can provide expert guidance to our clients and ensure that each study is backed by our trademark quality and diligence.

What AMPAR Antagonists Can We Develop?

• Competitive AMPAR antagonists
• Non-competitive AMPAR antagonists

Screening of Compounds Targeting AMPAR

We use high-throughput screening and molecular modeling to help clients quickly identify compounds with the potential to modulate AMPAR activity. Once a lead compound is identified, we apply medicinal chemistry and computational chemistry techniques to optimize its properties and convert it into a lead compound. This process involves iterative design, synthesis, and testing to improve potency, selectivity, and other desirable properties. In addition, we perform early ADME (absorption, distribution, metabolism, excretion, and toxicity) and PK (pharmacokinetics) assessments for AMPAR antagonists.

Preclinical Evaluation for AMPAR Antagonists

Ace Therapeutics partners with the world's pharmaceutical and biotechnology companies. Innovative and rigorous science, excellence in execution and absolute integrity, coupled with a flexible model, enable Ace Therapeutics to deliver valuable results in a relatively short period of time.

Efficacy Testing of AMPAR Antagonist in Animal Models of Stroke

Our team of neuroscientists continues to develop the most relevant in vivo stroke models and assays to help you evaluate the therapeutic potential of AMPAR antagonists. We use our expertise in pharmacology, biochemistry and molecular biology to design and conduct studies to measure the impact of AMPAR antagonists on stroke-related biomarkers and endpoints.

Safety Assessment of AMPAR Antagonists

Our deep expertise in pharmacology and pathology allows us to design and conduct comprehensive studies to measure the potential effects of AMPAR antagonists on the central nervous system to ensure a full understanding of the safety of AMPAR antagonists. Our approach is designed to reduce risk, minimize time delays and reduce costs associated with the advancement of AMPAR antagonists.

Ace Therapeutics offers reliable AMPAR antagonist development services to pharmaceutical companies focused on stroke drug development. Through our comprehensive preclinical evaluation, optimization and formulation strategies, DMPK studies and collaborative approach, we are committed to advancing the stroke therapy through the development of novel and effective AMPAR antagonists. If you are interested in our services, please do not hesitate to contact us!

1. Suda, S., & Kimura, K. (2019). Therapeutic potential of AMPA receptor antagonist perampanel against cerebral ischemia: beyond epileptic disorder. Neural Regeneration Research, 14(9), 1525-1526.