A2A Receptor Antagonists and Parkinson’s Disease Treatment

You can find out more about NPF’s National Medical Director, Dr. Michael S. Okun, by also visiting the NPF Center of Excellence, University of Florida Center for Movement Disorders & Neurorestoration.
One of the exciting recent changes in the treatment approach to Parkinson’s disease has been the development of new brain targets that have attempted to move the field beyond the typical dopamine and dopamine agonist-based treatments. One of the brain targets that has gleaned tremendous interest from multiple pharmaceutical companies, as well as from leading scientists from around the world, has been the adenosine A2 receptor. In this month’s What’s Hot column, I will review what is known about this brain receptor, and also provide an update on the status of clinical trials focused on the A2A receptor antagonists for treatment of Parkinson’s disease.
What is the adenosine A2A receptor? There is a group of circuits in the brain called the basal ganglia that are collectively involved in the underlying problems that result in the symptoms of Parkinson’s disease. The basal ganglia have a ton of adenosine A2A receptors located on the outside of nerve cells that are referred to as neurons. Many of these receptors have been observed to be co-located next to dopamine receptors. Scientists believe that you can either activate the dopamine receptor, or alternatively block the adenosine A2 receptor as a means to improving the symptoms of Parkinson’s disease. There has been some speculation that this class of drugs may when used in combination with dopaminergic drugs (e.g. levodopa and agonists) facilitate a reduction in the dosage of dopamine, and a coincident reduction in side effects.

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