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  • Title: Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists.
    Author: Nieto MI, Balo MC, Brea J, Caamaño O, Cadavid MI, Fernández F, Mera XG, López C, Rodríguez-Borges JE.
    Journal: Bioorg Med Chem; 2009 May 01; 17(9):3426-32. PubMed ID: 19346133.
    Abstract:
    In order to identify a high-affinity, selective antagonist for the A(2B) subtype adenosine receptor, more than 40 1,8-disubstituted-3-(3-methoxypropyl) xanthines were prepared and evaluated for their binding affinity at recombinant human adenosine receptors, mainly of the A(2A) and A(2B) subtypes. Some of the 1-ethyl-3-(3-methoxypropyl)-8-aryl substituted derivatives 15(a-m) showed moderate-to-high affinity at human A(2B) receptors, with compound 15d showing A(2B) selectivity over the other A receptors assayed (A(1), A(2A), A(3)) of 34-fold or over.
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