From Wikipedia, the free encyclopedia
Chemical compound
ADX-71149
ATC code
1-Butyl-3-chloro-4-(4-phenylpiperidin-1-yl)-1,2-dihydropyridin-2-one
CAS Number
PubChem
CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Formula C 20 H 25 Cl N 2 O
Molar mass 344.88 g·mol−1 3D model (
JSmol )
CCCCN1C=CC(=C(C1=O)Cl)N2CCC(CC2)C3=CC=CC=C3
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
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
[update] , ADX-71149 is in
phase II clinical trials for
schizophrenia .
[4]
See also
References
^ 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 .
^ 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 .
^ 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 .
^
a
b 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 .
^ 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 .
^ 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 .
External links
Group I
mGluR1 Tooltip Metabotropic glutamate receptor 1
mGluR5 Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2 Tooltip Metabotropic glutamate receptor 2
mGluR3 Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4 Tooltip Metabotropic glutamate receptor 4
mGluR6 Tooltip Metabotropic glutamate receptor 6
mGluR7 Tooltip Metabotropic glutamate receptor 7
mGluR8 Tooltip Metabotropic glutamate receptor 8