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Submit ReviewNPS 2390 is a group I mGlu antagonist; displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. Thought to act on a site separate from the glutamate binding pocket.
NPS 2390 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 | 307.39 |
公式 | C19H21N3O |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 226878-01-9 |
PubChem ID | 7067728 |
InChI Key | ZKFVOZCCAXQXBU-UHFFFAOYSA-N |
Smiles | O=C(C4=NC(C=CC=C5)=C5N=C4)NC1(CC3C2)CC(C3)CC2C1 |
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 | 15.37 | 50 | |
ethanol | 15.37 | 50 |
以下数据基于产品分子量 307.39。 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 |
---|---|---|---|
0.5 mM | 6.51 mL | 32.53 mL | 65.06 mL |
2.5 mM | 1.3 mL | 6.51 mL | 13.01 mL |
5 mM | 0.65 mL | 3.25 mL | 6.51 mL |
25 mM | 0.13 mL | 0.65 mL | 1.3 mL |
参考文献是支持产品生物活性的出版物。
Lavreysen et al (2003) [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. Mol.Pharmacol. 63 1082 PMID: 12695537
Mabire et al (2005) Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 48 2134 PMID: 15771457
van Wagenen et al (2000) Structure-activity relationship studies of NPS 2390: a potent and selective group I metabotropic glutamate receptor antagonist. Abstr.Soc.Neurosci. Program No. 618.3.
If you know of a relevant reference for NPS 2390, please let us know.
关键词: NPS 2390, NPS 2390 supplier, NPS2390, type, I, metabotropic, glutamate, mglu, mglur1, mglur5, antagonists, Glutamate, (Metabotropic), Group, Receptors, 4134, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NPS 2390 的部分引用包括:
Lezmy et al (2021) Astrocyte Ca 2+-evoked ATP release regulates myelinated axon excitability and conduction speed. Science 374 eabh2858 PMID: 34648330
Li et al (2016) Calcium Oxalate Induces Renal Injury through Calcium-Sensing Receptor. Oxid Med Cell Longev 2016 5203801 PMID: 27965733
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NPS 2390 was used as a specific blocker of mGluR1 and mGluR5, to isolate pharmacologically response of GABA-A receptors. 10 microM of NPS 2390 in perfusion solution generated a full block of mGluR group I receptor activity, thus leaving a clear GABA-ergic response. Figure: single-channel openings of GABA-A receptor after application of NPS 2390.
Compound requires sonication to be dissolved.
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.
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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.