NYX-2925 – (2012536-16-0)

NYX-2925 is an orally active N-methyl-D-aspartate receptor (NMDAR) modulator designed to restore levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the medial prefrontal cortex (mPFC). This compound exhibits a unique pharmacological profile, showing no effect on CAMKII and lacking addictive or sedative/ataxic side effects, which makes it a promising candidate for research into various NMDA receptor-mediated central nervous system disorders.

In clinical trials, NYX-2925 has demonstrated a favorable safety and tolerability profile. A first-in-human, phase I study involving 84 healthy adult volunteers showed that NYX-2925 was safe and well-tolerated, with dose-proportional pharmacokinetics and minimal accumulation after once-daily dosing for seven days. The study also confirmed that NYX-2925 crosses the blood-brain barrier, with maximum cerebrospinal fluid concentrations approximating 6-9% of maximum plasma concentrations at the same dose level.

NYX-2925 is being developed for the treatment of chronic pain conditions, including painful diabetic peripheral neuropathy and fibromyalgia. Preclinical studies have shown that it induces rapid and long-lasting analgesia in rat models of neuropathic pain, suggesting its potential as a novel therapeutic agent for chronic pain management.

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Sources:

https://pubchem.ncbi.nlm.nih.gov/compound/122594417
https://www.medchemexpress.com/nyx-2925.html
https://www.medkoo.com/products/50819
https://pubmed.ncbi.nlm.nih.gov/30242962/
https://www.sciencedirect.com/science/article/pii/S2590098620300543