A_2A Adenosine Receptor Antagonists and Their Efficacy in Rat Models of Parkinson's Disease.

ABSTRACT: Parkinson's disease (PD) represents a growing challenge to global health, as it involves millions of people. The high grade of disability is due to the loss of dopaminergic neuron activity, and levodopa is the gold-standard therapy used to restore dopamine in the dopamine-denervated regions. Another therapeutic approach is the use of A_2A adenosine receptor antagonists and, among them, istradefylline is the only one currently approved for therapy in association with levodopa. In this work, we synthesized A_2A adenosine receptor antagonists represented by 9-ethyl-2,8-disubstituted adenine derivatives, which were tested at human adenosine receptors in binding and functional assays. These compounds showed A_2A adenosine receptor-binding affinities in the low nano

SUBMITTER: Spinaci A 

PROVIDER: S-EPMC11898488 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature