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


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 A2A-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 A2A 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.

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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.

Conflicts of Interest

The authors declare no conflicts of interest.


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