Adenosine radioligand binding studies

In a search for more potent and selective Ai adenosine receptor agonists, and taking in mind that at Ai receptor the most active analogues were substituted adenosines, a series of N -cycloalkyl-1-deazaadenosine derivatives were synthesized and evaluated in radioligand binding studies and adenylate cyclase assays [13]. N -Cyclopentyl-2-chloro-1-deazaadenosine (1-deazaCCPA) showed the highest affinity at Ai receptor with more than two fold higher Ai selectivity than N -cyclopentyladenosine (CPA). 

---