| Stereochemistry | RACEMIC |
| Molecular Formula | C13H16N2O |
| Molecular Weight | 216.2789 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1(CC2=C(O1)C=CC=C2)C3=NCCN3
InChI
InChIKey=RATZLMXRALDSJW-UHFFFAOYSA-N
InChI=1S/C13H16N2O/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13/h3-6H,2,7-9H2,1H3,(H,14,15)
Efaroxan (RX 821037) is a potent and selective alpha(2)-adrenoceptor antagonist. Additionally, Efaroxan is a selective antagonist at the imidazoline I1 receptor. Efaroxan promotes insulin secretion, in the absence of exogenous agonists, by a mechanism that involves inhibition of ATP-regulated K+ channels.
Efaroxan was in clinical trials for the treatment of diabetes mellitus however its development has been discontinued.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 4.4 nM [Ki] | |||
| 52.36 nM [Ki] |
PubMed
Patents
ACTIVE MOIETY
