Trapidil
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Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.
Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.
Trapidil is thought to inhibit cyclic adenosine monophosphate (cAMP) phosphodiesterase enzymes . The resultant increase in cAMP potentiates the inhibition of platelets by adenosine . The reduction in platelet activation is likely responsible for the decrease in thromboxane A2 generation seen with trapidil . The increase in cAMP is also likely responsible for the vasdilatory action of trapidil. The increase in protein kinase A activity due to increased cAMP activated L-type calcium channels in the heart leading to increased depolarization and a positive inotropic effect . Lastly, PKA inactivates Raf-1, an activator of mitogen activated protein kinase (MAPK), which leads to a reduction in MAPK activation. This reduction in MAPK prevents mitogenesis due to PDGF binding to PDGF receptors .
Used in the treatment of chronic stable angina .
