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Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A1 and A2 Adenosine-Receptor Antagonists in Rats
- Source :
- Pharmacology & Pharmacy. :303-311
- Publication Year :
- 2013
- Publisher :
- Scientific Research Publishing, Inc., 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.
Details
- ISSN :
- 21579431 and 21579423
- Database :
- OpenAIRE
- Journal :
- Pharmacology & Pharmacy
- Accession number :
- edsair.doi...........0cb60616d9ced2ee7dab50fbaa395916