| 货号 | 2079/50 |
| 别名 | (S)-1-(2-Amino-2-carboxyethyl)-3-(2 |
| 供应商 | Tocris |
| 生物活性 | Potent and selective GLUK5 (GluR5)-subunit containing kainate receptor antagonist (apparent KD = 402 nM); active enantiomer of UBP 296 (Cat. No. 2078). Displays ~ 260-fold selectivity over AMPA receptors, ~ 90-fold selectivity over recombinant human GLUK6- and GLUK2-containing kainate receptors and has little or no action at NMDA or group I mGlu receptors. Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers. Also protects against soman-induced seizures and neuronal degeneration for up to 30 days when administered one hour after soman exposure. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 333.3 |
| 分子式 | C15H15N3O6 |
| 可溶性/溶解性 | Soluble to 25 mM in 1eq. NaOH and to 20 mM in DMSO with gentle warming |
| 参考文献 | Aplandet al (2014) The Limitations of Diazepam as a Treatment for Nerve Agent-Induced Seizures and Neuropathology in Rats: Comparison with UBP302. J.Pharmacol.Exp.Ther. 351 359. PMID: 25157087. Dolmanet al (2005) Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J.Med.Chem. 48 7867. PMID: 16302825. Moreet al (2004) Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology 47 46. PMID: 15165833. |