COMPARATIVE PHARMACOLOGY OF NUCLEOSIDE TRANSPORT INHIBITORS

The few existing nucleoside transport inhibitors are almost equipotent on the transporter in washed human erythrocytes. Large differences exist however in tightness of binding and activity in the presence of human plasma, as well as in ex vivo inhibition and duration of action when given intravenously or orally. Examples are presented of the marked effect of nucleoside transport inhibition on adenosine accumulation in ischemic myocardium. That may explain the remarkable cardioprotection in several models when a nucleoside transport inhibitor with an appropriate pharmacokinetic profile (such as R 75 231) is applied.