NMDA Receptor Antagonist Development for Stroke

The N-methyl-D-aspartate receptor (NMDAR) is a glutamate-gated ion channel that underlies the physiology and pathology of the mammalian central nervous system. Activation of NMDAR leads to the activation of inward calcium currents and downstream cell death signaling, which in turn leads to the aberrant activation of many calcium-dependent enzymes in the brain, initiating necrosis, apoptosis, and autophagy processes. In recent decades, the study of NMDAR and its downstream cell signaling activation has become a hotspot of neuronal injury mechanisms in ischemic stroke.

Fig. 1. Perturbing the NMDA receptor can protect neurons from ischemic injury. Fig. 1. Perturbing the GluN2B-PSD95-nNOS complex protects neurons from ischemic injury. (Wu et al., 2018)

Our NMDAR Antagonist Development Services

At Ace Therapeutics, we are at the forefront of preclinical stroke drug development services. Our extensive experience and expertise in this field can help clients develop more effective and safer NMDAR antagonists. In addition, we can design and develop new drugs that target the downstream pathways of the NMDAR to selectively block NMDAR-mediated synaptic transmission.

Our fully equipped laboratories have advanced equipment for molecular biology, cell culture, drug screening, and imaging facilities. These allow us to perform complex experiments and generate reliable data to support the development of NMDAR antagonists for the treatment of stroke.

Screening of Compounds Targeting NMDAR and Its Downstream Pathways

We use robust computational modeling and high-throughput screening techniques to rapidly screen for drugs that can bind to multiple regulatory sites in the NMDAR complex and target the pro-death pathway downstream of NMDA. In addition, we can help clients discover new targets based on the analysis of NMDAR and its downstream signaling pathways of ischemic cell death.

Developing stroke drugs that bind to multiple NMDAR regulatory sites	Targeting glycine and glutamate binding sites Targeting ion channel Targeting the NR2B subunit Targeting polyamine regulatory site
Developing stroke drugs that target NMDAR downstream pro-death pathway	Targeting GluN2B-PSD95-nNOS complex Targeting PSD95 Targeting GluN2B-DAPK1-p53 complex Targeting GluN2B NMDAR-PTEN Targeting NMDAR-SFK-Panx1 Targeting Calpain (NCX3, kidin220, STEP, mGluR1) Targeting MAPK (p38, JNK)

Preclinical Evaluation Services for NMDAR Antagonists

To advance the pharmacological research on NMDAR antagonists with the support of Ace Therapeutics. Our team combines stroke expertise with extensive knowledge of molecules, modalities, and stroke model systems to create a mature portfolio of in vitro and in vivo stroke models to support your pharmacological studies and deepen your understanding of new stroke therapies.

Ace Therapeutics is a leading stroke drug development company providing reliable NMDAR antagonist development services to clients worldwide. Our integrated approach ensures seamless NMDAR antagonist development. This integrated model streamlines the development process, enabling efficient decision-making and accelerating the development process. If you are interested in our services, please do not hesitate to contact us!

Reference

Wu, Q. J., & Tymianski, M. (2018). Targeting NMDA receptors in stroke: new hope in neuroprotection. Molecular brain, 11, 1-14.

All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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