Author(s)

Ilhuicamina Daniel Limón-Pérez de León, María del Carmen Parra-Cid, Alejandro Muñoz-Zurita, Saúl Alejandro Merino-Contreras, Sara Montiel-Smith, Socorro Meza-Reyes, Gerardo Ramírez-Mejía, Jesús Sandoval-Ramírez

Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México.
Instituto Nacional de Rehabilitación, Unidad de Ingeniería de Tejidos, Terapia Celular y Medicina Regenerativa, México DF, México.

A series of 1,3-substituted 8-styrylxanthines (11a-d) was synthesized, under chemo- and regioselective conditions, in a good overall yield. The compounds showed affinity towards both A₁ and A_2A-adenosine receptors by radioligand binding by means of in vitro assays. The (E)-3-ethyl-1-propyl-8-styrylxanthine (11a) showed the greatest affinity towards the A_2A receptor, whereas (E)-3-pentyl-1-propyl-8-styrylxanthine (11d) showed the greatest affinity for the A₁ receptor. When the 8-styrylxanthines 11a (A15Et) and 11c (A15Bu) were administrated in rats, which were previously injured with 6-hydroxydopamine at the substantia nigra pars compacta (SNc), the turning behavior decreased 50%. Based on these results we propose to A15Et as a potential compound to treat some symptoms of Parkinson’s disease.

Xantines; Adenosine Receptors Antagonists; Turning Behavior; Anti-Parkinsonian Drugs

I. León, M. Parra-Cid, A. Muñoz-Zurita, S. Merino-Contreras, S. Montiel-Smith, S. Meza-Reyes, G. Ramírez-Mejía and J. Sandoval-Ramírez, "Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A₁ and A₂ Adenosine-Receptor Antagonists in Rats," Pharmacology & Pharmacy, Vol. 4 No. 3, 2013, pp. 303-311. doi: 10.4236/pp.2013.43044.