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LY 456236 hydrochloride
Biological Activity for LY 456236 hydrochloride
LY 456236 hydrochloride is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). Reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.
Technical Data for LY 456236 hydrochloride
|Storage||Desiccate 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.
Solubility Data for LY 456236 hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for LY 456236 hydrochloride
The following data is based on the product molecular weight 317.77. 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|
|0.2 mM||15.73 mL||78.67 mL||157.35 mL|
|1 mM||3.15 mL||15.73 mL||31.47 mL|
|2 mM||1.57 mL||7.87 mL||15.73 mL|
|10 mM||0.31 mL||1.57 mL||3.15 mL|
Product Datasheets for LY 456236 hydrochloride
References for LY 456236 hydrochloride
References are publications that support the biological activity of the product.
Shannon et al (2005) Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology 49 188 PMID: 16011839
Bertorelli et al (2005) Selective blockade of metabotropic glutamate subtype mGluR1 receptors induce anti-nociceptive effects. Neuropharmacology 49 231
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Citations for LY 456236 hydrochloride
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Reviews for LY 456236 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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1 microM LY 456236 was tested on action potentials generated by current injection into CA3 hippocampal neuron. Application of LY increased significantly a number of action potentials. This effect disappeared after partial block of NMDA receptors. Illustration: control recording of action potentials (top) and recording with LY 456236 (bottom).
Can be easily diluted, no problem with long-time storage in aliquots.
Literature in this Area
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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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Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
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.