Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A<sub>1</sub> and A<sub>2</sub> Adenosine-Receptor Antagonists in Rats — Oak Academic Publishing
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Motor Effects of 1,3-Disubstituted 8-Styrylxanthines as A<sub>1</sub> and A<sub>2</sub> Adenosine-Receptor Antagonists in Rats
Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Instituto Nacional de Rehabilitación, Unidad de Ingeniería de Tejidos, Terapia Celular y Medicina Regenerativa, México DF, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
1 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
2 Instituto Nacional de Rehabilitación, Unidad de Ingeniería de Tejidos, Terapia Celular y Medicina Regenerativa, México DF, México
3 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
4 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
5 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
6 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
7 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
8 Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, México
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 A 1 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 A 1 receptor. When the 8-styrylxanthines 11a (A15Et) and 11c (A15Bu) were administrated in rats, which were previously injured with 6-hydroxydopamine at the su bstantia 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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