Trapidil is used in the treatment of chronic stable angina pectoris. It is currently marketed in Japan under the brand name Rocornal.
An analog was assigned the codename AR 12-456.
Based on cell free in vitro activity assays, trapidil at therapeutic concentrations causes selective phosphorylation of cellular proteins through positive modulation of regulatory subunit RII(ñ/ò) containing protein kinase A (PKA). At higher, non-physiologically relevant concentrations, which are generally not achieved after administration of therapeutic doses, non-selective inhibition of phosphodiesterases occurs. Further, the previous documented activities as an antagonist of platelet-derived growth factor are abolished when a PKA inhibitor is administered, suggesting that these noted activities are PKA mediated. At these higher concentrations, additional effects have been noted including vasodilation and inhibition of platelet aggregation