Hidden Pockets In NMDA Receptor Discovered For Stroke, Seizure Treatment

When it comes to ideal drugs the basic function is to affect the specific neurons and exact cells designed for a specific treatment with no unnecessary side effects. This theory comes into reality when it comes to treating complex and subtle human brain. Recently, a group of researchers from the Cold Spring Harbor Laboratory has found a method that can help time-consuming specific treatments of strokes and seizures. According to Professor Hiro Furukawa, chemistry plays an important role when it comes to treating specific diseases and also creating target-specific drugs.

The human brain generally gets injured during a stroke which results in part of the brain acidifying. The acidification process results in the abundant release of glutamate. The glutamate starts spreading across the entire place and hits the N-methyl, D-aspartate (NMDA) receptor which later starts firing some more of it. The NMDA receptor in a normal brain generally deals with managing and controlling the course of the electrically stimulated ions or atoms in and out of the neurons. The memory formation and learning are effected on a large scale from the firing signals.  The overexpression of the neurons can have detrimental effects. In the various neurological diseases and disorders, the abnormal NMDA receptor activities have a huge role to play like in the cases of Alzheimer’s disease, stroke, depression, seizure, and even in few of the genetic mutations. The researchers have found a way to prevent over-firing NMDA receptors without hampering the nearby brain regions.

In the earlier studies, the compounds named the 93-series were found to be perfect for the current purpose. In an acidic environment, the compound could join the NMDA receptor and bring about a downregulation in the receptor activity in the company of glutamate, thus inhibiting undue neuronal firing. The 93-series compounds in some cases cause superfluous consequence by inhibiting the NMDA receptors in the healthy regions of the brain. The features of the unique 93-series are currently being scrutinized. Using the X-ray crystallography, the 93-series compound motifs on a measly pocket in the NMDA receptor. This pocket has never been studied and shows pH sensitivity around it. The redesigned version named 94-series with a high pH sensitivity can attach to the NMDA receptors’ pockets and bring about the needed treatment. Ashok K. Shetty, a professor at the Texas A&M College of Medicine along with his team has developed GABAergic interneurons from the stem cells and later transplanted the human induced pluripotent stem cell-derived GABAergic progenitor cells in the hippocampus for eliminating the seizure or other cognitive effects.

Author: Hiren Sam