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Biological Activity for LY 354740
LY 354740 is a highly selective and potent agonist of group II mGlu receptors (EC50 values are 5.1 and 24.3 nM at mGlu2 and mGlu3 receptors respectively and > 100000 nM at mGlu4, mGlu7, mGlu1a and mGlu5a receptors). Displays antianxiety and antiaddictive activity in vivo. Orally and systemically active.
Technical Data for LY 354740
|Storage||Store at +4°C|
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.
Solubility Data for LY 354740
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for LY 354740
The following data is based on the product molecular weight 185.18. 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|
|1 mM||5.4 mL||27 mL||54 mL|
|5 mM||1.08 mL||5.4 mL||10.8 mL|
|10 mM||0.54 mL||2.7 mL||5.4 mL|
|50 mM||0.11 mL||0.54 mL||1.08 mL|
References for LY 354740
References are publications that support the biological activity of the product.
Schoepp et al (1997) LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cell expressing human glutamate receptors. Neuropharmacology 36 1 PMID: 9144636
Helton et al (1998) Anxiolytic and side-effect profile of LY354740: a potent, highly selective, orally active agonist for group II metabotropic glutamate receptors. J.Pharmacol.Exp.Ther. 284 651 PMID: 9454811
Klodzinska et al (1999) Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models. Neuropharmacology 38 1831 PMID: 10608278
If you know of a relevant reference for LY 354740, please let us know.
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Keywords: LY 354740, LY 354740 supplier, Potent, selective, group, II, mGlur, agonists, Group, Receptors, mGlu2, mGluR2, mGlu3, mGluR3, Glutamate, Metabotropic, LY354740, (Metabotropic), 3246, Tocris Bioscience
5 Citations for LY 354740
Citations are publications that use Tocris products. Selected citations for LY 354740 include:
Copeland et al (2015) Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. Sci Rep 92 16 PMID: 25576798
Dornier (2017) Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells. Nat Commun 8 2255 PMID: 29269878
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Yaeger and Trussell (2015) Single granule cells excite Golgi cells and evoke feedback inhibition in the cochlear nucleus. J Neurosci 35 4741 PMID: 25788690
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Literature in this Area
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.
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.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Learning & Memory Poster
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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
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.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.