Diimidazo[1,2-c:4',5'-e]pyrimidines: Adenosine agonist activity demonstrated by microphysiometry

Article abstract of DOI:10.1016/S0960-894X(98)00102-4

Silicon-based microphysiometry, measuring extracellular acidification rate of cells in culture, demonstrated that a series of diimidazo[1,2-c:4',5'-e]pyrimidines were agonists at the human adenosine A₁ receptor. 5-amino-7,8-dihydro-3-ribofuranose-8-(R)-(phenyl)-3H-diimidazo[1,2-c:4',5' -e]pyrimidine (2a) had an EC₅₀ of 100 μM and reached 90% of the E(max) produced by R-PIA.