Proadifen
Proadifen is a non-selective inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism. It is also an inhibitor of neuronal nitric oxide synthase, CYP-dependent arachidonate metabolism, transmembrane calcium influx, and platelet thromboxane synthesis. Further documented effects include the blockade of ATP-sensitive inward rectifier potassium channel 8, and stimulation of endothelial cell prostacyclin production.
Proadifen exerts apoptotic/anti-proliferate effects in certain forms of cancer, believed to be caused by mediation of glycogen synthase kinase 3 β. In the same study administration of proadifen was demonstrated to produce time- and dose-dependent phosphatidylserine externalization, caspase-3 activation and PARP cleavage. Intense upregulation of NAG-1 and ATF3 and downregulation of Mcl-1 and Egr-1 were also observed.
Proadifen has been demonstrated to inhibit the nicotinic acetylcholine receptor and muscarinic acetylcholine receptor in rats.
