N(6)-SUBSTITUTED 2-PHENYL-9-BENZYL-8-AZAADENINES - AFFINITY FOR ADENOSINE A(1)-RECEPTOR AND A(2)-RECEPTOR - A COMPARISON WITH 2-N-BUTYL ANALOGOUS DERIVATIVES .5.
G. Biagi et al., N(6)-SUBSTITUTED 2-PHENYL-9-BENZYL-8-AZAADENINES - AFFINITY FOR ADENOSINE A(1)-RECEPTOR AND A(2)-RECEPTOR - A COMPARISON WITH 2-N-BUTYL ANALOGOUS DERIVATIVES .5., Il Farmaco, 49(3), 1994, pp. 187-191
The title compounds were prepared to evaluate their affinity towards a
denosine A1 and A2 receptors. Some 2-phenyl-N(6)-substituted-8-azadeni
nes showed good binding properties and good A1 selectivity. The biolog
ical results allow us to confirm the presence in A1 receptors of a thi
rd 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 a
nd 2-phenyl derivatives indicate that they arrange themselves within A
1 receptors in a similar manner and suggest that this receptor is able
to arrange 8-azaadenines, bearing three lipophilic substituents, in t
wo different ways.