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Author(s): José Enrique Rodríguez-Borges
Xerardo García-Mera
María Carmen Balo
José Brea
Olga Caamaño
Franco Fernández
Carmen López
María Isabel Loza
María Isabel Nieto
Title: Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists
Issue Date: 2010
Abstract: A number of novel xanthines bearing a variety of substituents at positions 1, 3, 7 and 8 were prepared andevaluated for their binding affinity to the human adenosine receptor A1, A2A, A2B and A3 subtypes. Severalof the 1,3,8- and 1,3,7,8-substituted xanthines showed moderate-to-high affinity at human A2B and A1receptors, with the most active compound (14q) having a pKi of 7.57 nM for hA2B receptors and a selectivityover hA2A receptors of 8.1-fold and hA1 receptors of 3.7-fold.
Subject: Química orgânica, Química clínica, Engenharia química
Organiz chemistry, Clinical chemistry, Chemical engineering
Scientific areas: Ciências da engenharia e tecnologias::Engenharia química
Engineering and technology::Chemical engineering
Document Type: Artigo em Revista Científica Internacional
Rights: restrictedAccess
Appears in Collections:FCUP - Artigo em Revista Científica Internacional

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