excitotoxicity

2-hexyl-4-Pentynoic Acid, a valproic acid (VPA) derivatives, is a potent and robust HDACs inhibitor with IC50 value of 13 μM.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

MSN-125 effectively inhibits Bax Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond

WMS-1405 is a derivative of ifenprodil. As a potent NR2B-selective NMDA receptor antagonist, it exhibits a Ki value of 5.4 nM. Synthesized through a central building block approach, WMS-1405 displays high NR2B affinity due to the specific distance between its basic nitrogen atom and phenyl residue. WMS-1405 has the potential to serve as an NMDA antagonist for excitotoxicity treatment.

MDAR IN-1 (Compound 5m) is a brain-penetrant acetylcholinesterase (AChE) inhibitor and an antagonist of the NMDAR receptor GluN1/GluN2B subtype. It effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR to reduce excitotoxicity. MDAR IN-1 shows potential for Alzheimer’s disease research.

FLY26 is a selective partial antagonist of GluN2B, with an IC50 value of 0.64 μM. FLY26 inhibits the GluN2B subunit of NMDA receptors, reducing calcium ion influx and reactive oxygen species (ROS) production. It also activates the BDNF/TrkB/CREB neuroprotective signaling pathway, mitigating excitotoxicity and mitochondrial dysfunction. FLY26 holds potential for treating neurological deficits caused by cerebral ischemia-reperfusion injury.

PD150606 is a selective nonpeptide calpain inhibitor with neuroprotective activity that inhibits μ-calpains and m-calpains. Inhibits erythrocyanine-induced Ca2+ efflux and interferes with excitotoxicity-dependent motor neuron death.

Selective TrkB receptor agonist. Protects neurons from excitotoxicity. Protects retinas from light-induced retinal degeneration (LIRD) in vivo. Blood brain barrier and blood-retinal barrier penetrant.

Sepimostat dimethanesulfonate (FUT-187), a chemical compound, demonstrates neuroprotective properties by antagonizing NR2B N-methyl-D-aspartate receptors at the NR2B subunit's Ifenprodil-binding site. This compound effectively inhibits Ifenprodil binding, exhibiting a Ki value of 27.7 μM[1].

5-(2-furyl)-N-propylisoxazole-3-carboxamide is a compound used as a molecular structural unit and is thought to be a modulator of NMDA receptors, and has been shown to be protective against glutamate-induced excitotoxicity and oxidative stress in neuronal cells. It has also been found to have anti-inflammatory activity, making it a potential therapeutic agent for diseases such as Alzheimer's disease and Parkinson's disease.

GTS511 is a EAAT2 Activator. Pharmacokinetic profiles (PK) of GTS511 show a >6 h half-life and higher bioavailability in plasma and the brain under all three routes of administration in rats. GTS511 can be further developed to treat neurological disorders caused by excitotoxicity

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.

TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, protecting neurons against oxidative stress and NMDAR-mediated excitotoxicity, making it valuable for neuroprotection research studies [1].

Ganglioside GM1 is one of the major sphingolipids (GSLs) on the cell surface of the central nervous system (CNS), which is protective of the CNS and is used in the study of neurological disorders.Ganglioside GM1 exerts protection against glutamate excitotoxicity through its oligosaccharides in wild-type and amyotrophic lateral sclerosis motor neurons.

PF-9601N showed high potency and selectivity as a MAO-BI (monoamine oxidase type B inhibitor) and also demonstrated remarkable neuroprotective properties in several in vivo and cellular models of PD.

Fraxinellone analog 1 (compound 2) is an effective and rapid activator of the Nrf2-mediated antioxidative defense system, providing protection against glutamate-mediated excitotoxicity. It induces the expression of antioxidative genes Gpx4, Sod1, and Nqo1. Additionally, Fraxinellone analog 1 exerts neuroprotective effects and modulates oxidative stress and inflammation, making it suitable for research on neurodegenerative diseases.

Neuroprotectin B is a cyclic peptide that safeguards cultured chicken neurons from excitotoxicity induced by glutamate and kainic acid.

Neuroprotectin A (Complestatin A) is a cyclic peptide that safeguards cultured chicken brain neurons from excitotoxicity caused by glutamate and kainic acid.

15-Methoxypinusolidic acid has anti-inflammatory effects, it inhibits LPS-induced iNOS expression and NO production, independent on MAPK and NF-kappaB. 15-Methoxypinusolidic acid suppresses adipocyte differentiation through the inhibition of PPARgamma-dep