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Submit ReviewSYM 2081
说明： Highly selective kainate agonist
化学名： (2S,4R)-4-Methylglutamic acid
纯度： ≥97% (HPLC)
生物活性 for SYM 2081
SYM 2081 is a potent and highly selective kainate receptor agonist, with an IC50 for inhibition of [3H]-kainate binding of 35 nM and almost 3,000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively. Also selectively inhibits the cloned excitatory amino acid transporter EAAT2 at higher concentrations.
许可信息
Sold with the permission of Annovis Inc.
技术数据 for SYM 2081
| 分子量 | 161.16 |
| 公式 | C6H11NO4 |
| 储存 | Store at RT |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 31137-74-3 |
| PubChem ID | 95883 |
| InChI Key | KRKRAOXTGDJWNI-DMTCNVIQSA-N |
| Smiles | [H][C@@](N)(C(O)=O)C[C@]([H])([C@](O)=O)C |
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.
产品说明书 for SYM 2081
参考文献 for SYM 2081
参考文献是支持产品生物活性的出版物。
Donevan et al (1998) The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors. J.Pharmacol.Exp.Ther. 285 539 PMID: 9580595
Jones et al (1997) Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate. Neuropharmacology 36 853 PMID: 9225313
Savidge et al (1999) Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells. Neuropharmacology 38 375 PMID: 10219975
Zhou et al (1997) (2S,4R)-4-Methylglutamic acid (SYM 2081): a selective, high affinity ligand for kainate receptors. J.Pharmacol.Exp.Ther. 280 422 PMID: 8996224
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关键词: SYM 2081, SYM 2081 supplier, inhibitors, inhibits, EAAT2, kainate, receptors, agonist, selective, EAAT, Excitatory, Amino, Acid, Transporters, GLT-1, Glutamate, Monoamine, Neurotransmitter, iGluR, Ionotropic, SYM2081, Kainate, Receptors, 0903, Tocris Bioscience
6 篇 SYM 2081 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SYM 2081 的部分引用包括：
Gangadharan et al (2011) Peripheral calcium-permeable AMPA receptors regulate chronic inflammatory pain in mice. J Clin Invest 121 1608 PMID: 21383497
Santos et al (2009) Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord. PLoS One 4 e8047 PMID: 19956641
Pollok and Reiner (2020) Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization Proc Natl Acad Sci USA 117 25851 PMID: 32999066
Yoshii et al (2013) A Myosin Va mutant mouse with disruptions in glutamate synaptic development and mature plasticity in visual cortex. Addict Biol 33 8472 PMID: 23658184
Vielma et al (2014) Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells. PLoS One 9 e114330 PMID: 25463389
Rojas et al (2013) Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors. Mol Pharmacol 83 106 PMID: 23066089
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