Molecules, Vol. 26, Pages 1188: Combined Therapy of A1AR Agonists and A2AAR Antagonists in Neuroinflammation

Molecules, Vol. 26, Pages 1188: Combined Therapy of A1AR Agonists and A2AAR Antagonists in Neuroinflammation Molecules doi: 10.3390/molecules26041188 Authors: Gabriella Marucci Diego Dal Ben Catia Lambertucci Aleix Martí Navia Andrea Spinaci Rosaria Volpini Michela Buccioni Alzheimer’s, Parkinson’s, and multiple sclerosis are neurodegenerative diseases relatedby neuronal degeneration and death in specific areas of the central nervous system. These pathologiesare associated with neuroinflammation, which is involved in disease progression, and haltingthis process represents a potential therapeutic strategy. Evidence suggests that microglia functionis regulated by A1 and A2A adenosine receptors (AR), which are considered as neuroprotective andneurodegenerative receptors, respectively. The manuscript’s aim is to elucidate the role of thesereceptors in neuroinflammation modulation through potent and selective A1AR agonists (N6-cyclopentyl-2′- or 3′-deoxyadenosine substituted or unsubstituted in 2 position) and A2AAR antagonists(9-ethyl-adenine substituted in 8 and/or in 2 position), synthesized in house, using N13 microglialcells. In addition, the combined therapy of A1AR agonists and A2AAR antagonists to modulate neuroinflammationwas evaluated. Results showed that A1AR agonists were able, to varying degrees,to prevent the inflammatory effect induced by cytokine cocktail (tumor necrosis factor (TNF)-α,interleukin (IL)-1β, and interferon (IFN)-γ), ...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research