ENIPORIDE

Description

Eniporide is a selective inhibitor of human Na⁺/H⁺ exchanger isoform 1 (NHE-1) (IC₅₀ = 4.5 nM). Inhibition with eniporide prevents calcium overload-induced myocardial ischemia-reperfusion injury in vitro and in vivo.

in vitro

eniporide was identified as a selective inhibitor of na+-h+ exchange and a compound of the benzoylguanidine group. in addition, eniporide and its metabolite were found to inhibit the na+-h+ exchange in acidified rabbit erythrocytes with an ic50 value of 4.7 ± 0.6 and 15 ± 3 nm, respectively [1].

in vivo

animal study showed that the pretreatment of the mice with the eniporide led to a substantial decrease of annexin-v–positive cardiomyocytes in the i/r 30/90 group from 20.2% to 2.2%. moreover, the pretreatment of i/r 30/90 mice with eniporide resulted in the complete absence of igg-positive cells, suggesting that the cardiomyocytes with extensive cell membrane leakage were a result of an active cell death program [2].

References

[1] bhattaram va, nagaraja nv, peters t, machnig t, kroesser s, kovar a, derendorf h. population pharmacokinetics of eniporide and its metabolite in healthy subjects and patients with acute myocardial infarction. j clin pharmacol. 2005 jun;45(6):631-9.
[2] dumont ea et al. cardiomyocyte death induced by myocardial ischemia and reperfusion: measurement with recombinant human annexin-v in a mouse model. circulation. 2000 sep 26;102(13):1564-8.