Design and synthesis of adenosine receptor antagonists

Adenosine receptors (AR) belong to the G-protein coupled receptor family. There are four receptor subtypes: A1, A2A, A2B e A3. Adenosine receptor subtypes show a different distribution in the organism and are implicated in several physiopathological processes. In particular, antagonists towards A1AR are promising in the treatment of cognitive disorders. A2A antagonists seem to be involved in decrease the neurological impairment observed in Parkinson’s disease. A2B antagonists are potential therapeutic agents in asthma and diabetes. Finally, antagonists at the A3AR could be implicated in tumor growth inhibition and in glaucoma treatment. The crystallographic structure acquisition of the human A2A receptor allowed the design of new AR antagonists by the help of computational techniques. Our group is focused on the synthesis of new adenosine receptor antagonists (particularly towards A2A and A3) for their potential therapeutic use, but also as tools for pharmacological investigations on these receptors.

Research Group

Prof. Spalluto's group
Last update: 06-14-2024 - 21:50