NYX-2925, A NOVEL, NON-OPIOID, SMALL-MOLECULE MODULATOR OF THE N-METHYL-d-ASPARTATE RECEPTOR (NMDAR), DEMONSTRATES POTENTIAL TO TREAT CHRONIC, SUPRASPINAL CENTRALIZED PAIN CONDITIONS

Gajda, Jessica Marie; Asiedu, Marina N.; Morrison, Gladys; Dunning, Jacqueline Ann; Ghoreishi-Haack, Nayereh; Barth, A

doi:10.1016/j.medidd.2020.100067

Cited by 3 publications

(2 citation statements)

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“…NYX-2925 is a mimetic of rapastinel [ 23 ]. The modulator has been tested in a rodent model of neuropathic pain before being developed for the treatment of fibromyalgia (NCT03219320, NCT04147858) [ 309 , 310 ]. Regarding NYX-458, its administration resulted in rapid and long-lasting improvement in cognitive function across the domains of attention, working memory, and executive function in a primate PD model.…”

Section: Modulators Of Nmdars For the Treatment Of Neurological Disor...mentioning

confidence: 99%

Targeting NMDA Receptors at the Neurovascular Unit: Past and Future Treatments for Central Nervous System Diseases

Seillier

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et al. 2022

IJMS

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The excitatory neurotransmission of the central nervous system (CNS) mainly involves glutamate and its receptors, especially N-methyl-D-Aspartate receptors (NMDARs). These receptors have been extensively described on neurons and, more recently, also on other cell types. Nowadays, the study of their differential expression and function is taking a growing place in preclinical and clinical research. The diversity of NMDAR subtypes and their signaling pathways give rise to pleiotropic functions such as brain development, neuronal plasticity, maturation along with excitotoxicity, blood-brain barrier integrity, and inflammation. NMDARs have thus emerged as key targets for the treatment of neurological disorders. By their large extracellular regions and complex intracellular structures, NMDARs are modulated by a variety of endogenous and pharmacological compounds. Here, we will present an overview of NMDAR functions on neurons and other important cell types involved in the pathophysiology of neurodegenerative, neurovascular, mental, autoimmune, and neurodevelopmental diseases. We will then discuss past and future development of NMDAR targeting drugs, including innovative and promising new approaches.

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Section: Modulators Of Nmdars For the Treatment Of Neurological Disor...mentioning

confidence: 99%

Targeting NMDA Receptors at the Neurovascular Unit: Past and Future Treatments for Central Nervous System Diseases

Seillier

Lesept

Toutirais

et al. 2022

IJMS

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show abstract

“…In the last paragraph on this page we mentioned that “Novel NMDA receptor antagonists like 19 , NYX-2925 ( 20 ), and RL-208 ( 21 ) were recently designed and synthesized (Figure 2); however, these compounds were not tested for activity in rodent pain models. − ” We would like to make the correction that, NYX-2925 is not an NMDA receptor antagonist but a glutamate coligand that positively modulates the NMDA receptor and binds all 4 NMDAR2A-D subtypes to facilitate channel opening even in the absence of glycine. NYX-2925 is currently in Phase II clinical development for the treatment of painful, diabetic peripheral neuropathy and fibromyalgia following extensive characterization in rodent models and may represent a unique mechanism for the treatment of chronic, supraspinal centralized pain conditions. − …”

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confidence: 99%