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A 841720Cat. No. 3060 |
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Chemical Name: 9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one |
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.Certificate of Analysis / Safety Data Sheet
References
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.
If you know of a relevant citation for this product please let us know.
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Keywords: A 841720, supplier, Selective, mGlu1, mGluR1, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, A841720
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