The AMPA subtype of glutamatergic receptors is the main actor in the excitatory neurotransmission in the mammalian central nervous system. These receptors are involved in the expression and the maintenance of the long-term potentiation, a phenomenon closely linked to cognitive and memorization processes.
Based on experimental data collected in recent years, the use of AMPA potentiators seems to be an interesting approach in the treatment of cognitive deficits (e.g. Alzheimer’s disease), schizophrenia or depression. Such AMPA signal potentiation could be mediated by positive allosteric modulators (PAMs) of the AMPA receptors, a class of compounds able to produce a fine signal tuning in the presence of the endogenous ligand in the synapse, providing less toxicity than direct agonists.
With this approach, the University of Liège developed many series of AMPA potentiators, among which 1,2,4-benzothiadiazine 1,1-dioxides (BTDs). The team is currently developing BTDs positive allosteric modulator radiolabeled with a fluorin-18 atom that can potentially be used in a clinical setting. For more information, click here.
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