Abstract
Importance of making available selective adenosine receptor antagonists
is boosted by recent findings of adenosine involvement in many CNS
dysfunctions. In the present work a series of 8-bromo-9-alkyl adenines
are prepared and fully characterized in radioligand binding assays
or functional cyclase experiments in respect to their interaction
with all the four adenosine receptor subtypes. Results show that
the presence of the bromine atom in 8-position of 9-substituted adenines
promotes in general the interaction with the adenosine receptors,
in particular at the A(2A) subtype. The present study also demonstrates
that adenine derivatives could be a good starting point to obtain
selective adenosine A(2B) receptor antagonists.
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