Mebudipine and Dibudipine: A Review

Based on QSAR studies two new DHP calcium-channel blockers, mebudipine and dibudipine, were synthesis and evaluated for their pharmacological activity in various tissues. These studies showed that, these compounds, with potency comparable or greater than that of nifedipine could relax the smooth muscles of various vascular tissues. Electrophysiological study showed that they antagonized calcium current in F1 neuronal soma membrane in Helix aspesa cells. Mebudipine has a greater time- and voltage-dependent inhibitory effect, as compared to nifedipine and this property could explain its prominent vaso-selective action. Based on pharmacokinetic studies it is found that these two compounds are extensively metabolized by hepatic cells and this will results in low bioavailability after oral administration. However, these newer 1,4-DHPs address the problem of the short half-life of nifedipine, and are metabolically stable, possess comparable pharmacological activity as nifedipine and are therefore suitable for further development as potential therapeutic alternatives to the existing 1,4-DHP calcium-channel blockers. Based on their vaso-selectivity and longer half-lives and negative chronotropic activity, It is concluded that they have a great potential for further development as a new drug.