The title compounds were prepared to evaluate their affinity towards adenosine A1 and A2 receptors. Some 2-phenyl-N(6)-substituted-8-azadenines showed good binding properties and good A1 selectivity. The biological results allow us to confirm the presence in A1 receptors of a third lipophilic pocket, able to receive the substituent on N(9), and to evince increased affinity when a phenyl group on C(2) substitutes an n-butyl group. These affinity differences between analogous 2-n-butyl and 2-phenyl derivatives indicate that they arrange themselves within A1 receptors in a similar manner and suggest that this receptor is able to arrange 8-azaadenines, bearing three lipophilic substituents, in two different ways.
N(6)-substituted 2-phenyl-9-benzyl-8-azaadenines. Affinity for adenosine A1 and A2 receptors. A comparison with 2-N-butyl analogous derivatives.5.
GIORGI, IRENE;LUCACCHINI, ANTONIO;MARTINI, CLAUDIA;
1994-01-01
Abstract
The title compounds were prepared to evaluate their affinity towards adenosine A1 and A2 receptors. Some 2-phenyl-N(6)-substituted-8-azadenines showed good binding properties and good A1 selectivity. The biological results allow us to confirm the presence in A1 receptors of a third lipophilic pocket, able to receive the substituent on N(9), and to evince increased affinity when a phenyl group on C(2) substitutes an n-butyl group. These affinity differences between analogous 2-n-butyl and 2-phenyl derivatives indicate that they arrange themselves within A1 receptors in a similar manner and suggest that this receptor is able to arrange 8-azaadenines, bearing three lipophilic substituents, in two different ways.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
