A 841720 is a potent, non-competitive mGluR-1 antagonist that displays 34-fold selectivity over mGluR-5 (IC50 values are 10 and 342 nM respectively). A 841720 displays no significant activity at a range of other GPCRs, ion channels and transporters. This compound also exhibits analgesic effects, decreases mechanical allodynia in models of neuropathic pain, and impairs cognitive function.
Zheng et al (2005) Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J.Med.Chem. 48 7374. 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. More et al (2007) Comparison of the mGluR1 antagonist A-841720 in rats models of pain and cognition. Behav.Pharmacol. 18 273.
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