Dr. Mohammad Qneibi, the Founder and Director of the Neuroscience lab at the Faculty of Medicine and Health Sciences, has collaborated with Dr. Mohammed Hawash from the Department of Pharmacy to unveil groundbreaking research in the field of neuroscience. Their joint effort has resulted in the publication of a research article titled “Deciphering the Biophysical Properties of Ion Channel Gating Pores by Coumarin–Benzodiazepine Hybrid Derivatives: Selective AMPA Receptor Antagonists” in the Molecular Neurobiology Journal, renowned for its expertise in neuroscience and boasting an impressive impact factor of 5.1 (Q1).

The primary aim of their study was to unravel the intricate relationship between the structure and activity of the compound, shedding light on the potential effects of altering side chains on negative allosteric modulation. The investigation yielded invaluable insights into the interaction between eight CD compounds and AMPA receptor subunits. Notably, while all compounds exhibited effective blockade, CD8 demonstrated unparalleled potency and selectivity towards AMPA receptor subunits.

CD8, CD6, and CD5 exerted significant influence on deactivation and desensitization rates, setting them apart from the other five chemicals. These variations in binding and inhibition of AMPA receptor subunits were attributed to structural disparities among the compounds. The positioning of the carboxyl group of CD8, specifically at the para position of the phenyl ring, emerged as a crucial factor in augmenting AMPA receptor affinity.

The implications of this research underscore the potential of pharmaceutical compounds designed to specifically target AMPA receptors, offering a promising avenue for facilitating negative allosteric modulation in neurological contexts.

The full research article can be accessed here.

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