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ADX-71149

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ADX-71149
Clinical data
ATC code
  • None
Identifiers
  • 1‑Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)‑pyridone
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H15ClFNO2
Molar mass343.779 g/mol g·mol−1
3D model (JSmol)
  • COC1=CC=C(C=C1)C2=CN(C(=O)C=C2)CC3=C(C=C(C=C3)Cl)F
  • InChI=1S/C19H15ClFNO2/c1-24-17-7-3-13(4-8-17)14-5-9-19(23)22(11-14)12-15-2-6-16(20)10-18(15)21/h2-11H,12H2,1H3
  • Key:VLTLVMNNIVBONY-UHFFFAOYSA-N

ADX-71149, also known as JNJ-4041183 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]

See also

References

  1. ^ Cid, José María; Tresadern, Gary; Duvey, Guillaume; Lütjens, Robert; Finn, Terry; Rocher, Jean-Philippe; Poli, Sonia; Vega, Juan Antonio; de Lucas, Ana Isabel; Matesanz, Encarnación; Linares, María Lourdes; Andrés, José Ignacio; Alcazar, Jesús; Alonso, José Manuel; Macdonald, Gregor J.; Oehlrich, Daniel; Lavreysen, Hilde; Ahnaou, Abdelah; Drinkenburg, Wilhelmus; Mackie, Claire; Pype, Stefan; Gallacher, David; Trabanco, Andrés A. (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, Hilde; Ahnaou, Abdellah; Drinkenburg, Wilhelmus; Langlois, Xavier; Mackie, Claire; Pype, Stefan; Lütjens, Robert; Le Poul, Emmanuel; Trabanco, Andrés A.; Nuñez, José María Cid (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, Hilde; Langlois, Xavier; Donck, Luc Ver; Nuñez, José María Cid; Pype, Stefan; Lütjens, Robert; Megens, Anton (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. ^ a b Walker, Adam G; Conn, P Jeffrey (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, John; Brandon, Nicholas J (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.
  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". Retrieved 24 May 2015.


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