Rolofylline (KW-3902) is a potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM.
Rolofylline (KW3902) displays 290-fold selectivity over A2AR.
Rolofylline (KW3902) antagonizes NECA-induced bradycardic response in anesthetized rats (0.1-1mg/kg), causes significant increases of urine volume and sodium excretion with little change of potassium excretion in saline-loaded normal rats (0.001-1 mg/kg).
