| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H13FN2 |
| Molecular Weight | 240.2755 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(C)=C(N)C(=N1)C#CC2=CC(F)=CC=C2
InChI
InChIKey=MEDCLNYIYBERKO-UHFFFAOYSA-N
InChI=1S/C15H13FN2/c1-10-8-11(2)18-14(15(10)17)7-6-12-4-3-5-13(16)9-12/h3-5,8-9H,17H2,1-2H3
| Molecular Formula | C15H13FN2 |
| Molecular Weight | 240.2755 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
ADX 10059 is a first-in-class reflux inhibitor that works by reducing activation of the metabotropic glutamate receptor 5 (mGluR5) through negative allosteric modulation (NAM). This approach may lead to a new class of drugs that addresses the causes of GERD rather than just the symptoms. ADX 10059 is a potent selective NAM of the mGluR5, with
an IC50 of 17.1 nM on hmGluR5 showing good selectivity
compared with > 65 other receptors, transporters, ion
channels and enzymes. ADX 10059 completed Phase IIb testing in gastroesophageal reflux disease (GERD) and migraine prevention, demonstrated significant potential in a non-human primate model of Parkinson's disease levodopa induced dyskinesia (PD-LID). However, Addex Pharmaceuticals announced the discontinuation of development of ADX 10059 in December 2009 due to liver enzyme changes.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 17.1 nM [IC50] | |||
| 17.1 nM [IC50] |
PubMed
Patents
Sample Use Guides
ADX 10059 120 mg twice-daily given for two weeks was well tolerated and the tolerability profile seen is compatible with use in the treatment of GERD.
Route of Administration:
Oral
