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Submit ReviewLY 379268
说明： Highly selective group II mGlu agonist
化学名： (1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
纯度： ≥99% (HPLC)
生物活性 for LY 379268
LY 379268 is a highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors. Provides protection against NMDA-mediated cell death in vitro and offers almost complete protection against CA1 hippocampal damage following global ischemia in gerbils. Orally and systemically active. LY379268 disodium salt also available.
许可信息
Sold under license from Eli Lilly and Company
技术数据 for LY 379268
| 分子量 | 187.15 |
| 公式 | C7H9NO5 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 191471-52-0 |
| PubChem ID | 10197984 |
| InChI Key | YASVRZWVUGJELU-MDASVERJSA-N |
| Smiles | [H][C@]12[C@]([C@H]2[C@@](O)=O)([H])[C@](N)([C@](O)=O)CO1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for LY 379268
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 3.74 | 20 | |
| 1eq. NaOH | 18.71 | 100 |
制备储备液 for LY 379268
以下数据基于产品分子量 187.15。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.34 mL | 26.72 mL | 53.43 mL |
| 5 mM | 1.07 mL | 5.34 mL | 10.69 mL |
| 10 mM | 0.53 mL | 2.67 mL | 5.34 mL |
| 50 mM | 0.11 mL | 0.53 mL | 1.07 mL |
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产品说明书 for LY 379268
参考文献 for LY 379268
参考文献是支持产品生物活性的出版物。
Bond et al (1999) LY379268, a potent and selective group II metabotropic glutamate receptor agonist, is neuroprotective in gerbil global, but not focal cerebral ischaemia. Neurosci.Lett. 273 191 PMID: 10515191
Bond et al (2000) Neuroprotective effects of LY379268, a selective mGlu2/3 receptor agonist: investigations into possible mechanisms of action in vivo. J.Pharmacol.Exp.Ther. 294 800 PMID: 10945827
Collado et al (2002) (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 agonist with anxiolytic properties. J.Med.Chem. 45 3619 PMID: 12166935
If you know of a relevant reference for LY 379268, please let us know.
关键词: LY 379268, LY 379268 supplier, selective, group, II, agonists, Group, Receptors, mGlu2, mGluR2, mGlu3, mGluR3, Glutamate, Metabotropic, LY379268, (Metabotropic), 2453, Tocris Bioscience
19 篇 LY 379268 的引用文献
引用文献是使用了 Tocris 产品的出版物。 LY 379268 的部分引用包括：
Moreno et al (2011) Maternal influenza viral infection causes schizophrenia-like alterations of 5-HT2A and mGlu2 receptors in the adult offspring. J Biol Chem 31 1863 PMID: 21289196
Wang et al (2013) Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. PLoS One 8 e61787 PMID: 23593498
Durand et al (2011) Reduced cAMP, Akt activation and p65-c-Rel dimerization: mechanisms involved in the protective effects of mGluR3 agonists in cultured astrocytes. PLoS One 6 e22235 PMID: 21779400
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
Scholler (2017) Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation. Nat Commun 8 1967 PMID: 29213077
Chandrasekaran et al (2017) mGluR2/3 activation of the SIRT1 axis preserves mitochondrial function in diabetic neuropathy. Ann Clin Transl Neurol 4 844 PMID: 29296613
Liberto et al (2011) mGluR2/3 agonist LY379268, by enhancing the production of GDNF, induces a time-related phosphorylation of RET receptor and intracellular signaling Erk1/2 in mouse striatum. Neuropharmacology 61 638 PMID: 21619889
Johnson (2017) Metabotropic glutamate receptor 2 inhibits thalamically-driven glutamate and DA release in the dorsal striatum. Neuropharmacology 117 114 PMID: 28159646
Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase. Sci Rep 3 926 PMID: 23378895
Kurita et al (2012) HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity. Nat Neurosci 15 1245 PMID: 22864611
Sekizawa et al (2009) A novel postsynaptic group II metabotropic glutamate receptor role in modulating baroreceptor signal transmission. J Neurosci 29 11807 PMID: 19776267
Vinkers et al (2012) Lifelong CRF overproduction is associated with altered gene expression and sensitivity of discrete GABA(A) and mGlu receptor subtypes. Psychopharmacology (Berl) 219 897 PMID: 21833506
Hinzman et al (2012) Disruptions in the regulation of extracellular glutamate by neurons and glia in the rat striatum two days after diffuse brain injury. J Neurotrauma 29 1197 PMID: 22233432
Chen et al (2010) The glutamatergic compounds sarcosine and N-acetylcysteine ameliorate prepulse inhibition deficits in metabotropic glutamate 5 receptor knockout mice. Psychopharmacology (Berl) 209 343 PMID: 20217053
Garcia et al (2010) Cortical regulation of striatal medium spiny neuron dendritic remodeling in parkinsonism: modulation of glutamate release reverses DA depletion-induced dendritic spine loss. Cereb Cortex 20 2423 PMID: 20118184
Bellesi and Conti (2010) The mGluR2/3 agonist LY379268 blocks the effects of GLT-1 upregulation on prepulse inhibition of the startle reflex in adult rats. Neuropsychopharmacology 35 1253 PMID: 20072121
Moreno et al (2012) Identification of three residues essential for 5-hydroxytryptamine 2A-metabotropic glutamate 2 (5-HT2A-mGlu2) receptor heteromerization and its psychoactive behavioral function. Front Mol Neurosci 287 44301 PMID: 23129762
Erlandson et al (2015) The Functional Organization of Neocortical Networks Investigated in Slices with Local Field Recordings and Laser Scanning Photostimulation. Psychopharmacology (Berl) 10 e0132008 PMID: 26134668
Carbonaro et al (2015) The role of 5-HT2A, 5-HT 2C and mGlu2 receptors in the behavioral effects of tryptamine hallucinogens N,N-dimethyltryptamine and N,N-diisopropyltryptamine in rats and mice. J Neurosci 232 275 PMID: 24985890
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