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NPS 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. Find out more about compound libraries available from Tocris.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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.
View all Glutamate (Metabotropic) Group I Receptor Antagonists
Keywords: NPS 2390, NPS 2390 supplier, NPS2390, type, I, metabotropic, glutamate, mglu, mglur1, mglur5, antagonists, Glutamate, (Metabotropic), Group, Receptors, 4134, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for NPS 2390 include:
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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
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Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
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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.