Molecular structure of LY404039, CAS Number: 635318-11-5
LY404039 (CAS 635318-11-5)
Alternate Names:
LY2140023
Application:
LY404039 is A potent agonist of human mGluR-2, mGluR-3 receptors with Ki of 149 nM, and 92 nM respectively
CAS Number:
635318-11-5
Molecular Weight:
235.22
Molecular Formula:
C7H9NO6S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
LY404039, also known as LY2140023, is a small molecule that functions as a selective positive allosteric modulator of the metabotropic glutamate receptor 2 (mGlu2). When LY404039 binds to the mGlu2 receptor, it enhances the receptor′s response to glutamate, the primary excitatory neurotransmitter in the central nervous system. This interaction leads to the activation of downstream signaling pathways, including the inhibition of cyclic adenosine monophosphate (cAMP) production and the modulation of intracellular calcium levels. By modulating these cellular processes, LY404039 ultimately influences synaptic transmission and neuronal excitability. The functional role of LY404039 as a positive allosteric modulator of mGlu2 highlights its potential to modulate cellular signaling and impact neuronal function.
LY404039 (CAS 635318-11-5) References
- Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039). | Rorick-Kehn, LM., et al. 2007. J Pharmacol Exp Ther. 321: 308-17. PMID: 17204749
- Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors. | Monn, JA., et al. 2007. J Med Chem. 50: 233-40. PMID: 17228865
- Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial. | Patil, ST., et al. 2007. Nat Med. 13: 1102-7. PMID: 17767166
- Glutamate agonists for schizophrenia stimulate dopamine D2High receptors. | Seeman, P. 2008. Schizophr Res. 99: 373-4. PMID: 18077139
- Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039). | Fell, MJ., et al. 2008. J Pharmacol Exp Ther. 326: 209-17. PMID: 18424625
- Neither typical nor atypical: LY404039 provides proof of concept that selective targeting of mGluR2/3 receptors is a valid mechanism for obtaining antipsychotic efficacy. | Lebois, EP. 2008. Curr Top Med Chem. 8: 1480-1. PMID: 19006848
- Glutamate agonist LY404,039 for treating schizophrenia has affinity for the dopamine D2(High) receptor. | Seeman, P. and Guan, HC. 2009. Synapse. 63: 935-9. PMID: 19588471
- Memantine-induced brain activation as a model for the rapid screening of potential novel antipsychotic compounds: exemplified by activity of an mGlu2/3 receptor agonist. | Dedeurwaerdere, S., et al. 2011. Psychopharmacology (Berl). 214: 505-14. PMID: 21057775
- Reduced cAMP, Akt activation and p65-c-Rel dimerization: mechanisms involved in the protective effects of mGluR3 agonists in cultured astrocytes. | Durand, D., et al. 2011. PLoS One. 6: e22235. PMID: 21779400
- Comparative analysis of the neurophysiological profile of group II metabotropic glutamate receptor activators and diazepam: effects on hippocampal and cortical EEG patterns in rats. | Siok, CJ., et al. 2012. Neuropharmacology. 62: 226-36. PMID: 21791219
- An agonist at glutamate and dopamine D2 receptors, LY404039. | Seeman, P. 2013. Neuropharmacology. 66: 87-8. PMID: 22884896
- The [18F]FDG μPET readout of a brain activation model to evaluate the metabotropic glutamate receptor 2 positive allosteric modulator JNJ-42153605. | Wyckhuys, T., et al. 2014. J Pharmacol Exp Ther. 350: 375-86. PMID: 24898267
- Relative contributions of presystemic and systemic peptidases to oral exposure of a novel metabotropic glutamate 2/3 receptor agonist (LY404039) after oral administration of prodrug pomaglumetad methionil (LY2140023). | Annes, WF., et al. 2015. J Pharm Sci. 104: 207-14. PMID: 25382826
- In vitro characterization of the bioconversion of pomaglumetad methionil, a novel metabotropic glutamate 2/3 receptor agonist peptide prodrug. | Moulton, RD., et al. 2015. Drug Metab Dispos. 43: 756-61. PMID: 25755052
Inhibitor of:
PAMCI.Activator of:
mGluR-2, and mGluR-3.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
LY404039, 5 mg | sc-364524 | 5 mg | $112.00 | |||
LY404039, 25 mg | sc-364524A | 25 mg | $418.00 |