A 841720

Cat. No. 3060

A 841720 C17H21N5OS [869802-58-4]

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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.

Technical Data

M.Wt:
343.45
Formula:
C17H21N5OS
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in ethanol
Purity:
>98 %
Storage:
Store at RT
CAS No:
869802-58-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

More et al (2007) Comparison of the mGluR1 antagonist A-841720 in rats models of pain and cognition. Behav.Pharmacol. 18 273. PMID: 17551319.

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.

Zheng et al (2005) Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J.Med.Chem. 48 7374. PMID: 16279797.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for A 841720 include:

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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