Following the controversial approval of the amyloid-beta antagonist treatment aducanumab, Spanish researchers at the University of Barcelona have been testing the LSL60101 compound, with the potential to treat Alzheimer’s disease and neuroinflammation.
According to their study, released in the European Journal of Medicinal Chemistry and the British Journal of Pharmacology, the testing of rodents yielded improvements in cognitive deficits and may prove to be beneficial for treating certain neurogenerative diseases.
“Recent findings unveil the pharmacological modulation of imidazoline I2 receptors (I2-IR) as a novel strategy to face unmet medical neurodegenerative diseases,” the study reads.
“In this work, we report the chemical characterization, three-dimensional quantitative structure-activity relationship (3D-QSAR) and ADMET in silico of a family of benzofuranyl-2-imidazoles that exhibit affinity against human brain I2-IR and most of them have been predicted to be brain permeable.”
Researchers uncovered a neuroprotective role when testing LSL60101, known as garsevil, through its reduction of apoptosis and modulation of oxidative stress.
Its use may be significant for combatting the formation of amyloid-beta plaques in the brain, potentially becoming a neuroinflammatory treatment for diseases like Alzheimer’s disease.
LSL60101 was even compared with donepezil, a commonly used drug treatment for cognitive deficits, with the combination of both demonstrating efficaciousness for the neurodegenerative disease.
“Everything points out to the fact that the interaction of this drug with its receptor is involved in the generation of proinflammatory molecules that would increase the ongoing neuroinflammation in the disease. Therefore, I2 ligands would contribute to reduce the inflammation and thus, would slow the progression of the disease,” researchers stated in their study.
