Synthesis of di- and tri-substituted adenosine derivatives and their affinities at human adenosine receptor subtypes.
The synthesis of 2-(hex-1-ynyl)adenosine derivatives substituted at the N6- and/or 5'-position was carried out on the basis that 2-(hex-1-ynyl)adenosine-5'-N-ethyluronamide (HENECA, 2) showed good affinity and different degree of selectivity for rat adenosine receptors. All new compounds were tested in radioligand binding and adenylyl cyclase assays with recently cloned human A1, A2A, A2B, and A3 adenosine receptors.
Volpini
R
R
Dipartimento di Scienze Chimiche, Università di Camerino, Italy.
Camaioni
E
E
Costanzi
S
S
Vittori
S
S
Klotz
K N
KN
Cristalli
G
G
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D011869:Radioligand Assay; D051381:Rats; D043705:Receptor, Adenosine A2A; D043704:Receptor, Adenosine A2B; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000187:drug effects* / Q000235:genetics; D011993:Recombinant Fusion Proteins / Q000187:drug effects; D014162:Transfection
D043705:Receptor, Adenosine A2A; D043704:Receptor, Adenosine A2B; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D011993:Recombinant Fusion Proteins; D000262:Adenylyl Cyclases; D000241:Adenosine