Adenosine A2A Receptor Antagonists

Jiang-Fan Chen, MD, PhD, is an Associate Professor in the Boston University Medical Campus--Departments of Neurology and Pharmacology and Experimental Therapeutics. Dr. Chen’s research focuses on the neurobiology of adenosine and the A2A adenosine receptor and the role they may play in the development and treatment of neuropsychiatric disorders. Dr. Chen has developed an A2A receptor knockout mouse model and couples this genetic approach with pharmacological manipulation to explore the pathophysiological role of A2A receptors in animal and cellular models of neuropsychiatric disorders. The knowledge derived from these studies may provide the neurobiological basis for rational development of A2A receptor agents as treatment strategies for neuropsychological disorders, ranging from Parkinson’s disease to drug addiction. Akihisa Mori, Ph.D., is a global expert for Adenosine receptor neuroscience as well as Parkinson’s disease, having more than 3 decades experience to work for pharmaceutical industry from basic science, exploratory and translational research to global clinical development, for antiparkinsonian therapeutics. As for adenosine receptor neuroscience, he has discovered a functional significance of Adenosine A2A receptor in the basal ganglia as well as the adenosine A2A receptor antagonism mode of action as antiparkinsonian therapy. Also, he has made global leadership to develop a first-in class adenosine A2A receptor antagonist, Istradefylline, delivering the product to successful approval in the US and Japan. He has previously participated to be the Editor for volume 119 (Adenosine Receptors in Neurology and Psychiatry) of International Review of Neurobiology.

• 1. A2A Adenosine Receptor Agonists, Antagonists, Inverse Agonists and Partial AgonistsKenneth A. Jacobson2. Chemistry – agonists, antagonists, partial agonists, inverse agonistsChrista Müller3. Functional roles of adenosine receptors – biochemistry and neuronal plasticityAna Sebastiao4. A2A and Depression Rodrigo Cunha5. A2AR and glial functionZhihua Gao6. The adenosine A2A receptor in the basal ganglia: expression in health and disease, heteromerization, functional selectivity and signalling Rafael Franco, Gemma Navarro and Eva Martinez-Pinilla7. How and why A2a receptor become to be a therapeutic target in Parkinson’s disease therapyPeter Jenner8. Development of A2a antagonists for Parkinson’s disease – clinical evaluation for motor and non-motor symptomsYasar Torres-Yaghi9. The role of A2AR in chemobrain and the potential therapeutic benefits of istradefyllineDetlev Boison and Mi-hyeon Jang10. Effects of adenosine A2A receptors on cognitive function in health and diseaseAnna G. Orr, Cinthia Garcia and Avital Licht-Murava11. A2a receptor and Sleep disturbance Michael Lazarus and Mustafa Korkutata12. Adenosine A2A signals and DystoniaMakio Takahashi13. Protective potential of caffeine and adenosine A2A adenosine receptor antagonism in LRRK2 Parkinson’s diseaseMichael Schwarzschild14. A2a antagonists and Alzheimer’s diseaseDavid Blum15. A2a receptors and ALS/MSZheng Wu16. A2AR and trauma/PTSDYuanguo Zhou