Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A<sub>1</sub>and A<sub>2</sub>Adenosine-Receptor Antagonists in Rats

• 作者: Alejandro Mu?oz-Zurita Gerardo Ramírez-Mejía Ilhuicamina Daniel Limón-Pérez de León Jesús Sandoval-Ramírez María del Carmen Parra-Cid Sara Montiel-Smith Saúl Alejandro Merino-Contreras Socorro Meza-Reyes
• 来源期刊: 药理与制药(英文)
• 学科: 医学
• 关键词: Xantines ADENOSINE RECEPTORS ANTAGONISTS TURNING Behavior Anti-Parkinsonian Drugs
• 年，卷（期）: 2013,（3）
• 页码范围: 303-311
• 页数: 9页
• 分类号: R73

摘要

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.