Abstract
8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble
A2A-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX
(3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited
high affinity to rat A2A-AR in submicromolar concentrations, and
were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives
were inactive at human A2B- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine
(13) or only a 7-methyl derivative (14) showed similar (13) or higher
(14) A2A affinity than 11a and 11b but showed no (13) or only a low
degree (14) of selectivity versus A1-, A2B-, and A3-AR. The A2A-selective
sulfostyryl-DMPX derivatives exhibit high water-solubility and may
be useful research tools for in vivo studies.
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