A-134974

Enzyme inhibitor

This adenosine and 5-iodotubercidin analogue (FWfree-base = 375.17 g/mol), also known as [(1’R,2’S,3’R,4’S)-2’,3’ dihydroxy-4’-aminocyclopentyl]-4- amino-5-iodopyrrolopyrimidine, is a potent adenosine kinase inhibitor, IC50 = 60 pM. Because the use of adenosine receptor agonists is plagued by dose-limiting cardiovascular side effects, there is great interest in developing adenosine kinase inhibitors (AKIs) as a means for raising steady-state adenosine concentrations. A-134974 reduces thermal hyperalgesia and depresses locomotor activity.