69089-39-0Relevant articles and documents
8-(Sulfostyryl)xanthines: Water-soluble A(2A)-selective adenosine receptor antagonists
Mueller, Christa E.,Sandoval-Ramirez, Jesus,Schobert, Ulrike,Geis, Uli,Frobenius, Wolfram,Klotz, Karl-Norbert
, p. 707 - 719 (1998)
8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble A(2A)-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX (3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited high affinity to rat A(2A)-AR in submicromolar concentrations, and were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives were inactive at human A(2B)- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine (13) and its 7-methyl derivative (14) showed similar (13) or higher (14) A(2A) affinity than 11a and 11b but showed no (13) or only a low degree (14) of selectivity versus A1-, A(2B)-, and A3-AR. The A(2A)-selective sulfostyryl-DMPX derivatives exhibit high water-solubility and may be useful research tools for in vivo studies. Copyright (C) 1998 Elsevier Science Ltd.