| Stereochemistry | ACHIRAL |
| Molecular Formula | C14H16N4O3S |
| Molecular Weight | 320.367 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C=C(C(=C1)N2C=CC=C2)S(C)(=O)=O)C(=O)NC(N)=N
InChI
InChIKey=UADMBZFZZOBWBB-UHFFFAOYSA-N
InChI=1S/C14H16N4O3S/c1-9-7-11(18-5-3-4-6-18)12(22(2,20)21)8-10(9)13(19)17-14(15)16/h3-8H,1-2H3,(H4,15,16,17,19)
Eniporide belongs to the new class of drugs that specifically inhibit the Sodium/hydrogen exchanger 1 (NHE-1) isoform, which is the predominant isoform in the cardiac myocytes. Extensive preclinical studies, in vitro and in animals, have suggested that NHE inhibition with eniporide before the onset of ischemia is a very effective and reproducible means of limiting the extent of infarction and that this agent provides protective benefit even when given just before reperfusion. Eniporide had been in phase II clinical trial for the treatment of myocardial infarction. Administration of the eniporide, before reperfusion therapy in patients with acute ST-elevation myocardial infarction, did not limit infarct size or improve clinical outcome.
Originator
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Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as victim
Sourcing
Sample Use Guides
Eniporide (3 uM) and/or lidocaine (200 uM) were administered during 5 min prior to 40 min of global ischemia of isolated rat hearts and 40 min of drug free reperfusion to block the Na( )/H( ) exchanger and the Na( ) channel, respectively. Lidocaine reduced the rise in [Na( )](i) during the first 10 min of ischemia, followed by a rise with a rate similar to the one found in untreated hearts. Eniporide reduced the ischemic Na( ) influx during the entire ischemic period. Administration of both drugs resulted in a summation of the effects found in the lidocaine and eniporide groups. Contractile recovery and infarct size were significantly improved in hearts treated with both drugs, although not significantly different from hearts treated with either one of them.
ACTIVE MOIETY
