Adenosine A2A Receptor Antagonists as Anti-Parkinson Drugs

Parkinson?s disease (PD) is the second most frequent degenerative disorder after Alzheimer?s disease. At present, there is no cure for PD. While many medications treat PD, none actually reverse the effects of the disease or cure it. People with PD therefore often must take a variety of medications to manage the disease?s symptoms. Four subtypes of adenosine receptors have been cloned: designated A1, A2A, A2B, and A3. Adenosine A2A receptors (A2AR) are found in high density in certain brain regions, such as striatum, nucleus accumbens, and olfactory tubercle. Therefore antagonists at the A2AR have been proposed as novel therapeutics for PD and may also be active as cognition enhancers, neuroprotective, anti-depressive, and analgesic drugs. Novel xanthine derivatives will be designed, synthesized and characterized applying a wide range of physicochemical techniques. The novel compounds are expected to antagonize the A2AR with high affinity and selectivity and furthermore exhibit suitable pharmacokinetic properties.