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Submit ReviewLY 404187 is a selective AMPA receptor positive allosteric modulator (IC50 values are 0.15, 0.21, 1.66 and 5.65 μM for GluA2i, GluA4i, GluA3i and GluA1i respectively). Potentiates glutamate and AMPA-evoked currents in prefrontal cortex (PFC) pyramidal neurons in vitro. Has no effect on NMDA- or kainate-evoked currents; also has no effect on K+ or Na+ ion channels. Potentiates PFC glutamatergic synaptic transmission in vitro and in vivo. Induces neurite growth in combination with (S)-AMPA (Cat. No. 0254) in SH-SY5Y human neuroblastoma cells in vitro. Also reduces MPTP-induced toxicity in mice. Brain penetrant.
LY 404187 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 342.46 |
公式 | C19H22N2O2S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 211311-95-4 |
PubChem ID | 9928016 |
InChI Key | HOQAVGZLYRYHSO-UHFFFAOYSA-N |
Smiles | N#CC1=CC=C(C2=CC=C(C(C)CNS(C(C)C)(=O)=O)C=C2)C=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 34.25 | 100 | |
ethanol | 17.12 | 50 |
以下数据基于产品分子量 342.46。 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 | 2.92 mL | 14.6 mL | 29.2 mL |
5 mM | 0.58 mL | 2.92 mL | 5.84 mL |
10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
参考文献是支持产品生物活性的出版物。
O'Neill et al (2004) Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur.J.Pharmacol. 486 163 PMID: 14975705
Quirk and Nisenbaum (2002) LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. 8 255 PMID: 12353058
Voss et al (2007) Molecular mechanisms of neurite growth with AMPA receptor potentiation. Neuropharmacology 52 590 PMID: 17101156
Baumbarger et al (2001) Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J.Pharmacol.Exp.Ther. 298 86 PMID: 11408529
If you know of a relevant reference for LY 404187, please let us know.
关键词: LY 404187, LY 404187 supplier, LY404187, selective, ampa, receptors, positive, allosteric, modulators, PAMs, GLUA1, GLUA2, GLUA3, GLUA4, GLUR1, GLUR2, GLUR3, GLUR4, parkinson, disease, depression, memory, AMPA, Receptors, 5297, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.