title: 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
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.
authors.affiliation: Dipartimento di Scienze Chimiche, University of Camerino, Via S. Agostino 1, 62032 Camerino, Italy.
authors.forename: Catia
authors.initials: C
authors.lastname: Lambertucci
authors.forename: Ippolito
authors.initials: I
authors.lastname: Antonini
authors.forename: Michela
authors.initials: M
authors.lastname: Buccioni
authors.forename: Diego
authors.initials: D
authors.lastname: Dal Ben
authors.forename: Dhuldeo D
authors.initials: DD
authors.lastname: Kachare
authors.forename: Rosaria
authors.initials: R
authors.lastname: Volpini
authors.forename: Karl-Norbert
authors.initials: KN
authors.lastname: Klotz
authors.forename: Gloria
authors.initials: G
authors.lastname: Cristalli
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D003198:Computer Simulation; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D008958:Models, Molecular; D043705:Receptor, Adenosine A2A / Q000378:metabolism; D043704:Receptor, Adenosine A2B / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D043705:Receptor, Adenosine A2A; D043704:Receptor, Adenosine A2B; D000225:Adenine