| 货号 | 15351-1mg |
| 描述 | LY379268 is a potent, brain permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.1 In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.1 In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.1 However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.2 LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.3 In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Monn, J.A.,Valli, M.J.,Massey, S.M., et al. Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): Identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors. J. Med. Chem. 42(6), 1027-1040 (1999). 2.Wang, M.-J.,Li, Y.-C.,Snyder, M.A., et al. Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. PLoS One 8(4), e61787 (2013). 3.Bond, A.D.,Jones, N.M.,Hicks, C.A., et al. Neuroprotective effects of LY379268, a selective mGlu2/3 receptor agonist: investigations into possible mechanism of action in vivo. J. Pharmacol. Exp. Ther. 294(3), 800-809 (2000). 4.Cartmell, J.,Perry, K.W.,Salhoff, C.R., et al. The potent, selective mGlu2/3 receptor agonist LY379268 increases extracellular levels of dopamine, 3,4-dihydroxyphenylacetic acid, homovanillic acid, and 5-hydroxyindole-3-acetic acid in the medial prefrontal cortex of the freely moving rat. J. Neurochem. 75(3), 1147-1154 (2000). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | 4 |
| 纯度 | ≥99% |
| 计算分子量 | 187.2 |
| 分子式 | C7H9NO5 |
| CAS号 | 191471-52-0 |
| 稳定性 | ≥ 1 year |
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