Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A₁ and A₂ Adenosine-Receptor Antagonists in Rats

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.

DOI: 10.4236/pp.2013.43044                

Abstract

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.

Keywords

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

Conflicts of Interest

The authors declare no conflicts of interest.

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