TITLE:
Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A1 and A2 Adenosine-Receptor Antagonists in Rats
AUTHORS:
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
KEYWORDS:
Xantines; Adenosine Receptors Antagonists; Turning Behavior; Anti-Parkinsonian Drugs
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.4 No.3,
June
4,
2013
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 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.