A 841720
Chemical Name: 9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Background References
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Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Zheng et al.
J.Med.Chem., 2005;48:7374 -
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.
El-Kouhen et al.
Br.J.Pharmacol., 2006;149:761 -
Comparison of the mGluR1 antagonist A-841720 in rats models of pain and cognition.
More et al.
Behav.Pharmacol., 2007;18:273
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Citations for A 841720
The citations listed below are publications that use Tocris products. Selected citations for A 841720 include:
2 Citations: Showing 1 - 2
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Glutamate secretion and metabotropic glutamate receptor 1 expression during Kaposi's sarcoma-associated herpesvirus infection promotes cell proliferation.
Authors: Veettil Et al.
PLoS Pathog 2014;10:e1004389
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Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
Authors: Rojas Et al.
Mol Pharmacol 2013;83:106
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