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 A2A subtype. The present study also demonstrates that adenine derivatives could be a good starting point to obtain selective adenosine A2B receptor antagonists.
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A(2A) and A(2B) receptors ligands
LAMBERTUCCI, Catia;ANTONINI, Ippolito;BUCCIONI, Michela;DAL BEN, DIEGO;VOLPINI, Rosaria;CRISTALLI, Gloria
2009-01-01
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 A2A subtype. The present study also demonstrates that adenine derivatives could be a good starting point to obtain selective adenosine A2B receptor antagonists.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
