3′-Amidated 3′-Deoxyxylofuranose Analogues of N⁶-⁻Cyclopentyladenosines: a New Class of Non-Xanthine Antagonists at the Adenosine A₁ Receptor.

Abstract

Full adenosine A₁ receptor agonists like CPA and other N ⁶-⁻substituted adenosine analogs have previously been shown to become partial agonists upon deletion of the 3′-hydroxyl moiety. The present study further explored the C-3′ site for modification. The modest affinity at A₁ and A_2a receptors found in the 3′-amido-3′-deoxyxyIofuranosyladenine series prompted us to synthesize the corresponding N ⁶-⁻cyclopentyl derivatives, which proved to exhibit potent antagonistic behaviour at the A₁ receptors. This represents a new perspective in the purinergic field.