JNJ-40411813

• CAT Number: I000482
• CAS Number: 1127498-03-6
• Molecular Formula: C20H25ClN2O
• Molecular Weight: 344.88
• Purity: ≥95%
• Target: mGlu2R
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 147 nM(EC50)
• IUPAC Name: 1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2-one
• 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
• InChIKey: HYOGJHCDLQSAHX-UHFFFAOYSA-N
• SMILES: ClC1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN(CCCC)C1=O

JNJ-40411813 (CAT: I000482) is a novel compound that acts as a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor. The mGlu2 receptor is a G-protein-coupled receptor found in the central nervous system and is involved in the regulation of neurotransmission. By binding to a specific site on the mGlu2 receptor, JNJ-40411813 enhances the receptor’s activity, leading to increased modulation of glutamate signaling. This modulation has the potential to affect various neurological processes and may have therapeutic implications for conditions such as schizophrenia and other psychiatric disorders.

Reference

1:Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men. Ahnaou A, de Boer P, Lavreysen H, Huysmans H, Sinha V, Raeymaekers L, Van De Casteele T, Cid JM, Van Nueten L, Macdonald GJ, Kemp JA, Drinkenburg WH.Neuropharmacology. 2016 Apr;103:290-305. doi: 10.1016/j.neuropharm.2015.11.031. Epub 2015 Dec 12. PMID: 26686390
2:Pharmacokinetic and pharmacodynamic characterisation of JNJ-40411813, a positive allosteric modulator of mGluR2, in two randomised, double-blind phase-I studies. Salih H, Anghelescu I, Kezic I, Sinha V, Hoeben E, Van Nueten L, De Smedt H, De Boer P.J Psychopharmacol. 2015 Apr;29(4):414-25. doi: 10.1177/0269881115573403. Epub 2015 Mar 3. PMID: 25735992
3:Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813. Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A.Pharmacol Res Perspect. 2015 Mar;3(2):e00097. doi: 10.1002/prp2.97. Epub 2015 Jan 30. PMID: 25692027 Free PMC Article
4:Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM.Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9. PMID: 25692015 Free PMC Article
5: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. Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, Poli S, Vega JA, de Lucas AI, Matesanz E, Linares ML, Andrés JI, Alcazar J, Alonso JM, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA.J Med Chem. 2014 Aug 14;57(15):6495-512. doi: 10.1021/jm500496m. Epub 2014 Jul 28. PMID: 25032784