st-1535 and Parkinson-Disease

st-1535 has been researched along with Parkinson-Disease* in 1 studies

Other Studies

1 other study(ies) available for st-1535 and Parkinson-Disease

Article	Year
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. Journal of medicinal chemistry, 2013, Jul-11, Volume: 56, Issue:13 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

Article

Year

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.

Journal of medicinal chemistry, 2013, Jul-11, Volume: 56, Issue:13

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