Potent, non-competitive mGlu1 receptor antagonist that displays 34-fold selectivity over mGlu5 (IC50 values are 10 and 342 nM respectively). Displays no significant activity at a range of other GPCRs, ion channels and transporters. Exhibits analgesic effects; decreases mechanical allodynia in models of neuropathic pain. Also impairs cognitive function.
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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.
References are publications that support the biological activity of the product.
Zheng et al (2005) Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J.Med.Chem. 48 7374 PMID: 16279797
El-Kouhen et al (2006) Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br.J.Pharmacol. 149 761 PMID: 17016515
More et al (2007) Comparison of the mGluR1 antagonist A-841720 in rats models of pain and cognition. Behav.Pharmacol. 18 273 PMID: 17551319
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Keywords: A 841720, A 841720 supplier, Selective, mGlu1, mGluR1, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, A841720, (Metabotropic), 3060, Tocris Bioscience
2 Citations for A 841720
Citations are publications that use Tocris products. Selected citations for A 841720 include:
Rojas et al (2013) Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors. Mol Pharmacol 83 106 PMID: 23066089
Veettil et al (2014) Glutamate secretion and metabotropic glutamate receptor 1 expression during Kaposi's sarcoma-associated herpesvirus infection promotes cell proliferation. PLoS Pathog 10 e1004389 PMID: 25299066
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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.
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.
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.