Inhibition of nucleoside uptake in human erythrocytes by a new series of compounds related to lidoflazine and mioflazine.
The zero-trans influx of uridine in human erythrocytes is inhibited by lidoflazine and analogs thereof. The concentrations required for inhibition of nucleoside transport were higher when the compounds were simultaneously added with uridine than upon preincubation of the inhibitors with the erythrocytes. R70380 proved to be the most active compound in this respect, its IC50 value being 13 nM after preincubation. Even the reference compounds nitrobenzylthioinosine and dilazep were remarkably more potent with preincubation; dipyridamole, however, was not.
Pirovano
I M
IM
Dept. of Medicinal Chemistry, Center for Bio-Pharmaceutical Sciences, Leiden, The Netherlands.
Van Belle
H
H
Ijzerman
A P
AP
D001693:Biological Transport, Active / Q000187:drug effects; D002317:Cardiovascular Agents / Q000494:pharmacology*; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008013:Lidoflazine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D008024:Ligands; D009705:Nucleosides / Q000097:blood*; D010879:Piperazines / Q000494:pharmacology*; D014529:Uridine / Q000378:metabolism
D002317:Cardiovascular Agents; D008024:Ligands; D009705:Nucleosides; D010879:Piperazines; C041518:mioflazine; D008013:Lidoflazine; D014529:Uridine