Abstract (EN):
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.
Language:
English
Type (Professor's evaluation):
Scientific
Contact:
xerardo.garcia@usc.es (X. García-Mera).