ADX-71149

ADX-71149, also known as JNJ-40411813 and JNJ-mGluR2-PAM, is a selective positive allosteric modulator of the mGlu2 receptor.[1][2][3] It is being studied by Addex Therapeutics and Janssen Pharmaceuticals for the treatment of schizophrenia.[4] It was also researched by these companies for the treatment of anxious depression (major depressive disorder with anxiety symptoms),[5] but although some efficacy was observed in clinical trials, it was not enough to warrant further development for this indication.[6] As of 2015, ADX-71149 is in phase II clinical trials for schizophrenia.[4]

ADX-71149
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 1-Butyl-3-chloro-4-(4-phenylpiperidin-1-yl)-1,2-dihydropyridin-2-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC20H25ClN2O
Molar mass344.88 g·mol−1
3D model (JSmol)
SMILES
  • CCCCN1C=CC(=C(C1=O)Cl)N2CCC(CC2)C3=CC=CC=C3
InChI
  • 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
  • Key:HYOGJHCDLQSAHX-UHFFFAOYSA-N

See also

References
  1. Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, et al. (August 2014). "Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor". Journal of Medicinal Chemistry. 57 (15): 6495–512. doi:10.1021/jm500496m. PMID 25032784.
  2. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, et al. (February 2015). "Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor". Pharmacology Research & Perspectives. 3 (1): e00096. doi:10.1002/prp2.96. PMC 4317228. PMID 25692015.
  3. Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A (March 2015). "Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813". Pharmacology Research & Perspectives. 3 (2): e00097. doi:10.1002/prp2.97. PMC 4324682. PMID 25692027.
  4. Walker AG, Conn PJ (February 2015). "Group I and group II metabotropic glutamate receptor allosteric modulators as novel potential antipsychotics". Current Opinion in Pharmacology. 20: 40–5. doi:10.1016/j.coph.2014.11.003. PMC 4318747. PMID 25462291.
  5. Dunlop J, Brandon NJ (February 2015). "Schizophrenia drug discovery and development in an evolving era: are new drug targets fulfilling expectations?". Journal of Psychopharmacology. 29 (2): 230–8. doi:10.1177/0269881114565806. PMID 25586401. S2CID 42542103.
  6. Addex Therapeutics (7 February 2014). "Addex Reports Top-line Data from ADX71149 Phase 2a Study in Patients with Major Depressive Disorder (MDD) with Significant Anxiety Symptoms". Archived from the original on 25 May 2015. Retrieved 24 May 2015.


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