For research use only. Not for therapeutic Use.
LY354740（Cat No.:I002294）is a selective agonist of the metabotropic glutamate receptor 2 (mGluR2), a G-protein-coupled receptor involved in modulating neurotransmitter release in the brain. It has been primarily investigated for its potential therapeutic effects in neurological and psychiatric disorders, including schizophrenia, anxiety, and depression. By activating mGluR2, LY354740 is believed to help regulate glutamate transmission, which is often dysregulated in these conditions. Research has shown promising results in preclinical and early clinical studies, suggesting it may help alleviate symptoms, but further trials are needed to fully assess its safety and efficacy.
| CAS Number | 176199-48-7 |
| Synonyms | (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid |
| Molecular Formula | C8H11NO4 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Solubility | DMSO: ＜ 1.9 mg/mL |
| Storage | Store at +4C |
| IC50 | 5.1 ± 0.3 nM (EC50) |
| IUPAC Name | (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid |
| InChI | InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1 |
| InChIKey | VTAARTQTOOYTES-RGDLXGNYSA-N |
| SMILES | C1C[C@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(C(=O)O)N |
| Reference | </br>1:The group II metabotropic glutamate receptor agonist LY354740 and the D2 receptor antagonist haloperidol reduce locomotor hyperactivity but fail to rescue spatial working memory in GluA1 knockout mice. Boerner T, Bygrave AM, Chen J, Fernando A, Jackson S, Barkus C, Sprengel R, Seeburg PH, Harrison PJ, Gilmour G, Bannerman DM, Sanderson DJ.Eur J Neurosci. 2017 Apr;45(7):912-921. doi: 10.1111/ejn.13539. Epub 2017 Mar 4. PMID: 28186680 Free PMC Article</br>2:Levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model of schizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY379268 and LY354740. Orlando R, Borro M, Motolese M, Molinaro G, Scaccianoce S, Caruso A, di Nuzzo L, Caraci F, Matrisciano F, Pittaluga A, Mairesse J, Simmaco M, Nisticò R, Monn JA, Nicoletti F.Neuropharmacology. 2014 Nov;86:133-44. doi: 10.1016/j.neuropharm.2014.07.009. Epub 2014 Jul 22. PMID: 25063582 </br>3:Reversal of novelty-induced hyperlocomotion and hippocampal c-Fos expression in GluA1 knockout male mice by the mGluR2/3 agonist LY354740. Procaccini C, Maksimovic M, Aitta-Aho T, Korpi ER, Linden AM.Neuroscience. 2013 Oct 10;250:189-200. doi: 10.1016/j.neuroscience.2013.07.010. Epub 2013 Jul 15. PMID: 23867766 </br>4:The mGlu2/3 Receptor Agonists LY354740 and LY379268 Differentially Regulate Restraint-Stress-Induced Expression of c-Fos in Rat Cerebral Cortex. Menezes MM, Santini MA, Benvenga MJ, Marek GJ, Merchant KM, Mikkelsen JD, Svensson KA.Neurosci J. 2013;2013:736439. doi: 10.1155/2013/736439. Epub 2013 Nov 19. PMID: 26317098 Free PMC Article</br>5:Group II mGluR agonist LY354740 and NAAG peptidase inhibitor effects on prepulse inhibition in PCP and D-amphetamine models of schizophrenia. Profaci CP, Krolikowski KA, Olszewski RT, Neale JH.Psychopharmacology (Berl). 2011 Jul;216(2):235-43. doi: 10.1007/s00213-011-2200-0. Epub 2011 Feb 16. PMID: 21327758 Free PMC Article</br>6:The intestinal absorption of a prodrug of the mGlu2/3 receptor agonist LY354740 is mediated by PEPT1: in situ rat intestinal perfusion studies. Eriksson AH, Varma MV, Perkins EJ, Zimmerman CL.J Pharm Sci. 2010 Mar;99(3):1574-81. doi: 10.1002/jps.21917. PMID: 19780137 </br>7:Comparison of the mGlu(5) receptor positive allosteric modulator ADX47273 and the mGlu(2/3) receptor agonist LY354740 in tests for antipsychotic-like activity. Schlumberger C, Pietraszek M, Gravius A, Klein KU, Greco S, Morè L, Danysz W.Eur J Pharmacol. 2009 Nov 25;623(1-3):73-83. doi: 10.1016/j.ejphar.2009.09.006. Epub 2009 Sep 16. PMID: 19765575 </br>8:In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268). Fell MJ, Perry KW, Falcone JF, Johnson BG, Barth VN, Rash KS, Lucaites VL, Threlkeld PG, Monn JA, McKinzie DL, Marek GJ, Svensson KA, Nelson DL.J Pharmacol Exp Ther. 2009 Dec;331(3):1126-36. doi: 10.1124/jpet.109.160598. Epub 2009 Sep 15. PMID: 19755662 Free Article</br>9:Effects of a metabotropic glutamate receptor group II agonist LY354740 in animal models of positive schizophrenia symptoms and cognition. Schlumberger C, Schäfer D, Barberi C, Morè L, Nagel J, Pietraszek M, Schmidt WJ, Danysz W.Behav Pharmacol. 2009 Feb;20(1):56-66. doi: 10.1097/FBP.0b013e3283242f57. PMID: 19179851 </br>10:Transepithelial transport of the group II metabotropic glutamate 2/3 receptor agonist (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY354740) and its prodrug (1S,2S,5R,6S)-2-[(2/’S)-(2/’-amino)propionyl]aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY544344). Varma MV, Eriksson AH, Sawada G, Pak YA, Perkins EJ, Zimmerman CL.Drug Metab Dispos. 2009 Jan;37(1):211-20. doi: 10.1124/dmd.108.022012. Epub 2008 Oct 6. PMID: 18838508 Free Article |
