Abstract (EN):
The synthesis of an important set of 3-furfurylxanthine derivatives is described. Binding affinities were determined for rat A(1) and human A(2A), A(2B) and A(3) receptors. Several of the 3-furfuryl-7-methylxanthine derivatives showed moderate-to-high affinity at human A(2B) receptors, the most active compound (10d) having a K(i) of 7.4 nM for hA(2B) receptors, with selectivities over rA(1) and hA(2A) receptors up to 14-fold and 11-fold, respectively. Affinities for hA(3) receptors were very low for all members of the set.
Language:
English
Type (Professor's evaluation):
Scientific
Contact:
molga.caamano@usc.es; franco.fernandez@usc.es
No. of pages:
6