1224569-11-2Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists
Rodríguez-Borges, José Enrique,García-Mera, Xerardo,Balo, María Carmen,Brea, José,Caama?o, Olga,Fernández, Franco,López, Carmen,Loza, María Isabel,Nieto, María Isabel
scheme or table, p. 2001 - 2009 (2010/05/02)
A number of novel xanthines bearing a variety of substituents at positions 1, 3, 7 and 8 were prepared and evaluated for their binding affinity to the human adenosine receptor A1, A2A, A2B and A3 subtypes. Several of the 1,3,8- and 1,3,7,8-substituted xanthines showed moderate-to-high affinity at human A2B and A1 receptors, with the most active compound (14q) having a pKi of 7.57 nM for hA2B receptors and a selectivity over hA2A receptors of 8.1-fold and hA1 receptors of 3.7-fold.
