st-1535 has been researched along with Parkinson-Disease* in 1 studies
1 other study(ies) available for st-1535 and Parkinson-Disease
Article | Year |
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Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
The synthesis and preliminary in vitro evaluation of five metabolites of the A2A antagonist ST1535 (1) are reported. The metabolites, originating in vivo from enzymatic oxidation of the 2-butyl group of the parent compound, were synthesized from 6-chloro-2-iodo-9-methyl-9H-purine (2) by selective C-C bond formation via halogen/magnesium exchange reaction and/or palladium-catalyzed reactions. The metabolites behaved in vitro as antagonist ligands of cloned human A2A receptor with affinities (Ki 7.5-53 nM) comparable to that of compound 1 (Ki 10.7 nM), thus showing that the long duration of action of 1 could be in part due to its metabolites. General behavior after oral administration in mice was also analyzed. Topics: Adenine; Adenosine A2 Receptor Antagonists; Animals; Behavior, Animal; Binding, Competitive; CHO Cells; Cricetinae; Cricetulus; HEK293 Cells; Humans; Mice; Models, Chemical; Molecular Structure; Parkinson Disease; Radioligand Assay; Receptor, Adenosine A2A; Time Factors; Triazoles | 2013 |