| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H25ClN2O |
| Molecular Weight | 344.878 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCN1C=CC(N2CCC(CC2)C3=CC=CC=C3)=C(Cl)C1=O
InChI
InChIKey=HYOGJHCDLQSAHX-UHFFFAOYSA-N
InChI=1S/C20H25ClN2O/c1-2-3-12-23-15-11-18(19(21)20(23)24)22-13-9-17(10-14-22)16-7-5-4-6-8-16/h4-8,11,15,17H,2-3,9-10,12-14H2,1H3
JNJ-40411813 (aka ADX71149) is a metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator (PAM) that has the potential to be the first oral non-dopaminergic drug that may address both the positive and negative symptoms of schizophrenia and other indications, such as anxiety. ADX71149 is differentiated from marketed antipsychotics in that it may also show efficacy on negative symptoms and avoid compliance-limiting side effects such as weight gain, hyperprolactinemia and extrapyramidal symptoms, which are associated with the use of dopamine antagonists. The development of ADX71149 is part of a worldwide research collaboration and license agreement between Addex and Janssen Pharmaceuticals, Inc. This drug was also investigated for use as an adjunctive treatment for major depressive disorder (MDD), however, these studies were discontinued. JNJ-40411813 is now in phase II clinical trial for the treatment of epilepsy.
CNS Activity
Originator
Approval Year
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
PubMed
Patents
Sample Use Guides
Schizophrenia patients with residual negative symptoms would benefit most from treatment with ADX-71149 (JNJ-40411813), at a dose of 100 mg/day bid, as an adjunctive therapy to antipsychotics
Route of Administration:
Oral
JNJ-40411813 acts as a positive allosteric modulator at the cloned mGlu2 receptor: EC50 = 147 ± 42 nmol/L in a [(35)S]GTPγS binding assay with human metabotropic glutamate type 2 (hmGlu2) CHO cells and EC50 = 64 ± 29 nmol/L in a Ca(2+) mobilization assay with hmGlu2 G α16 cotransfected HEK293 cells.
ACTIVE MOIETY
