Neuroprotective effects of an BBB permeable phenoxythiophene sulfonamide small molecule in glutamate-induced oxidative injury.

Reactive oxygen species (ROS) play a central role in oxidative stress-associated neuronal cell death during ischemia. Further investigation into the inhibition of excessive ROS generation post-stroke is urgently required for the treatment of ischemic stroke. In the present study, the neuroprotective properties of the blood-brain barrier (BBB) penetrant B355227 were investigated.

Phenoxythiophene sulfonamide compound B355252 protects neuronal cells against glutamate-induced excitotoxicity by attenuating mitochondrial fission and the nuclear translocation of AIF.

Glutamate neurotoxicity has been implicated in the initiation and progression of various neurological and neurodegenerative disorders. Therefore, it is necessary to develop therapeutics for the treatment of patients with these devastating diseases. Mitochondrial fission plays an import role in the mediation of cell death and survival.

The Chemical Molecule B355252 is Neuroprotective in an In Vitro Model of Parkinson's Disease.

6-Hydroxydopamine (6-OHDA) is a neurotoxin frequently used to create in vitro and in vivo experimental models of Parkinson's disease (PD), a chronic neurodegenerative disorder largely resulting from damage to the nigrostriatal dopaminergic pathway. No effective drugs or therapies have been developed for this devastating disorder, and current regimens of symptomatic therapeutics only alleviate symptoms temporarily. Therefore, effective treatments that reverse or cure this disorder are urgently needed.

A novel phenoxy thiophene sulphonamide molecule protects against glutamate evoked oxidative injury in a neuronal cell model.

Background: Glutamate is one of the major neurotransmitters in the central nervous system. It is a potent neurotoxin capable of neuronal destruction through numerous signal pathways when present in high concentration. Glutamate-evoked excitotoxicity has been implicated in the etiology of many neurodegenerative diseases including Alzheimer's disease (AD), Parkinson's disease (PD), and ischemic stroke.