Irreversible inhibitors of adenosine receptors

摘要

Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based on 8-aryl-substituted xanthines as antagonists and on N6-substituted adenosine as agonists, wherein the electrophlic group may be, for example, isothiocyanate and N-hydroxysuccinimide esters.